Colloidal Drug Delivery Systems Research Articles

Review on Vesicular Drug Delivery System: Aquasomes

A special surface modification approach serves as a basis for a colloidal drug delivery system (CDDS) that helps to preserve the surface's constraining function. An aquasome is a submicronic structure (diameter 60-300nm). In order to create a medication delivery method other than liposome technology, they attracted a lot of attention in an effort to resolve issues with these vesicles' stability in biological fluids. Pharmaceuticals are absorbed by the aquasome, a molecular carrier made of a ceramic core (colloidal precipitation) to which glassy carbohydrates are subsequently permitted to adsorb as a nanometer-thick surface coating. Pharmaceuticals and other biochemically reactive surface members with non-covalently attached immobilized elements are stabilized by the carbohydrate coating, which also serves as a dehydroprotectant. These are nanoparticulate carrier systems but instead of being simple nanoparticles these are three layered self-assembled structures, comprised of a solid phase nanocrystalline core coated with oligomeric film to which biochemically active molecules are adsorbed with or without modification. These structures are self-assembled by non-covalent and ionic bonds. A large number of In vitro and animal model studies have been used to investigate the physical characteristics of this enabling system. It can be used as a carrier for vaccinations, hemoglobin, medications, dyes, enzymes, and even genetic material, giving it a very broad range of applications.

A brief review on basic fundamentals of nanoparticle (NPs)

According to studies made by previous researchers there are various technical problems associated with liposomes which can be avoided by designing colloidal drugs carrier like nanoparticles with nanotechnology. Now a days they are beneficial in the field of agriculture, veterinary, pharmaceutical, textile technologies. Site specific delivery of encapsulated drugs can be formulated with a nanometer size range which can be injected into the general circulation. The objective of this review is to explain the potential of NPs and nanotechnology associated with their characters and classifications, synthesis and application as the emerging scopes for NPs, rather will attract everyone’s attention. The aim of the present work is to characterize biodegradable nanoparticulate systems for oral controlled release, while numerous publications have appeared on this by international research teams, the research on polymeric nanoparticles has been primarily performed by a few research groups in Europe. Nanoparticles are being investigated as an alternative colloidal drug delivery system that could potentially avoid some of the technical problems observed with other drug delivery system.

Self emulsifying drug delivery system: norfloxacin model drug

Background Norfloxacin is a synthetic antibacterial fluoroquinolone that is poorly water soluble and active against a wide spectrum of gram-positive and gram-negative aerobic bacteria. The goal of this work was to create a self-nanoemulsion (SNE) as a colloidal dispersed drug delivery system for increasing norfloxacin dissolving rate, while also assuming intestinal lymphatic transport participation for such a nano-size system that would increase norfloxacin oral bioavailability. Methods Depending on the solubility of norfloxacin in various components, several formulations of liquid SNEDDS of the antibiotic were created using oleic acid (oil), tween20 (surfactant), and PEG200 (co-surfactant). To assess the presence of a nanoemulsion region, phase diagram was generated at various oil: surfactant: co-surfactant ratios. Results The in-vitro dissolution profile suggested an optimum norfloxacin SEDD formulation (F1) comprised of oleic acid (10%), tween 20 (45%), and PEG200 (45%), as opposed to commercially available traditional tablets. The F1 formula exhibited thermodynamic stability with a zeta potential of +60.78mV and a droplet size of 57.4nm. The F1 formula revealed an improved dissolving profile as compared to the commercial Tablet of norfloxacin. Conclusion Based on the findings, this study indicated that preparing norfloxacin as a liquid self-nanoemulsifying system improved the solubility and drug release of norfloxacin counteract the inconsistent bioavailability of the commercial tablet.

Preparation, Optimization, Characterization, and Evaluation of Rosuvastatin Loaded Solid Lipid Nanoparticles Using Quality by Design Approach

The present research work aims to prepare and characterize solid lipid nanoparticles (SLN) containing rosuvastatin calcium (RT). We aim to use a novel microwave-assisted microemulsion technique to produce Rosuvastatin-loaded SLN. The characterization of the optimized formulation of RTSLN was carried out by employing Fourier-transformed infrared spectroscopy (FTIR) and Differential scanning calorimetry (DSC) studies showed that there was no chemical interaction between drug (Rosuvastatin Calcium) and lipid (GMS), XRD indicated the amorphization of RTSLN formulation. In contrast, scanning electron microscopy (SEM) studies indicated that Rosuvastatin Calcium loaded SLNs are spherical, discrete, and homogeneous. In vitro and ex vivo drug release studies showed sustained drug release action. The effect of dependent variables such as entrapment efficiency (EE), particle size, and independent variables like % GMS and Poloxamer 407 was observed using a 32-factorial design approach. Optimized formulation was selected based on the 2D & 3D counter and surface response plots. The prepared formulations show percentage entrapment efficiency within the range of 53 to 78%, particle size in the 254.2 to 863.4 nm, and in vitro drug release was found to be 79.8%. Also, ex vivo absorption was 76.7 % for 8 hours. The need of the research work is to use microwave energy over conventional heating to prepare SLNs also helps to resolve problems associated with conventional colloidal drug delivery systems, which leads to improved drug bioavailability.

A Compendium of Bioavailability Enhancement via Niosome Technology.

Bioavailability is the dissimilarity between the total amount of drug exposure to a person and the actual dose received by his body. The difference in bioavailability between formulations of a given drug can have clinical implications. Poor aqueous solubility, inappropriate partition coefficient, high first-pass metabolism, narrow absorption window, and acidic pH of the stomach are the main reasons behind the low bioavailability of drugs. There are three substantial methods to vanquish these bioavailability issues, namely pharmacokinetic, biological, and pharmaceutical approaches. In the pharmacokinetic approach a drug molecule is improved by making alterations in its chemical structure. In the biological approach, the course of administration of the drug is changed; for example, if a drug has very less oral bioavailability, it can be injected as parenteral or some other route if feasible. In the pharmaceutical approach to enhance bioavailability, the physiochemical properties of the drug or formulation are modified. It is cost-effective, less time-consuming, and the risk factor is also minimum. Co-solvency, particle size reduction, hydrotrophy, solid dispersion, micellar solubilisation, complexation, and colloidal drug delivery systems are some of the commonly used methods to enhance the dissolution profiles of drugs via the pharmaceutical approach. Similar to liposomes, niosomes are also vesicular carrier systems but non-ionic surfactants are used instead of phospholipids in their formulation, i.e., their bilayer is comprised of non-ionic surfactants that encircle the aqueous compartment. The niosomes are presumed to raise the bioavailability of poorly water-soluble drugs by increasing their uptake by the M cells present in Peyer's patches of lymphatic tissues of the intestine. Niosomal technology has become an attractive method to overcome several limitations due to its various merits like biodegradability, high stability, non-immunogenic nature, low cost, and flexibility to incorporate lipophilic as well as hydrophilic drugs. The bioavailability of many BCS class II and IV drugs has been successfully enhanced using niosomal technology, like Griseofulvin, Paclitaxel, Candesartan Cilexetil, Carvedilol, Clarithromycin, Telmisartan, and Glimepiride. Niosomal technology has also been exploited for brain targeting via nasal delivery for many drugs like Nefopam, Pentamidine, Ondansetron HCl, and Bromocriptine mesylate. Based on this data, it can be concluded that niosomal technology has increased importance in bioavailability enhancement and improving the overall performance of molecules in vitro and in vivo. Thus, niosomal technology holds tremendous potential for scale-up applications, overcoming the drawbacks of conventional dosage forms.

Colloidal Drug Delivery of Simvastatin for Prolonged Drug Release and Increased Bioavailability

Hyperlipidemia is the major cause of atherosclerosis in which the lipid level in the blood plasma increases which leads to the formation of atherosclerotic plaque in the blood stream. Antihyperlipidemic drugs are used to reduce the high level of lipids and lipoproteins in the blood. HMG CoA reductase (Statin drugs) are the most potent group of antihyperlipidemic drugs and it works by inhibiting the Hydroxymethylglutaryl-coenzyme A (HMG CoA) reductase enzyme in the cholesterol synthesis. The most commonly used drug for decreasing low density lipoprotein (LDL) cholesterol is simvastatin. I is more efficacious as compared to Atorvastatin in increasing high density lipoprotein (HDL) cholesterol level. Simvastatin (SIM) is lipophilic in nature and is a perfect candidate for a novel colloidal drug delivery system (CDDS). CDDS delivers the drug to its target site to enhance the control release and to achieve the maximum therapeutic effect. This concept of targeting includes the nanoparticulate system such as Liposomes, Solid lipid nanoparticles (SLNs), Polymeric nanoparticles, Niosomes, Nanoemulsion and Metallic nanoparticles.

A colloidal hydrogel-based drug delivery system overcomes the limitation of combining bisphosphonates with bioactive glasses: in vitro evidence of a potential selective bone cancer treatment allied with bone regeneration

Bisphosphonates are a class of drugs that induce bone cancer cell death and favor bone regeneration, making them suitable for bone cancer treatment. However, when combined with bioactive glasses to enhance bone regeneration, a chemical bond between biphosphonates and the glass surface inactivates their mechanism of action. A new colloidal hydrogel-based drug delivery system could overcome that limitation once bisphosphonates, such as zoledronic acid (ZA), are incorporated into hydrogel micelles, avoiding their interaction with the glass surface. In this work, we proposed formulations based on a poloxamer 407 thermo-responsive hydrogel matrix containing holmium-doped bioactive glass nanoparticles and different concentrations (0.05 and 5 mg/mL) of ZA. We characterized the influence of the glass and the ZA on the hydrogel properties. In addition, a drug concentration screening was performed, and biological characterizations evaluated the best result. The biological characterization consisted of evaluating cytotoxicity and in vitro bone regeneration ability through cell migration and quantification of genes related to osteogeneses through RT-PCR. The results suggest that the addition of glasses and ZA to the poloxamer did not significantly influence the sol-gel transition of the hydrogels (around 13 °C) regardless of the ZA content. However, the ZA at high concentration (PL-ZA100) decreased the enthalpy of gel formation from 68 to 43 kJ.mol−1 when compared with the pure hydrogel formulation (PL), suggesting a water structurer role of ZA, which is withdrawn when glass particles are added to the system (PL-BG5Ho-ZA100). Solid-state 31P nuclear resonance spectroscopy results showed that part of the ZA is chemically bonded to the glass surface, which explains the withdrawal in the water structurer role of ZA when the glasses were incorporated into the hydrogel. Besides, based on the drug release results, we proposed a model where part of the ZA is “free,” encapsulated in the hydrogel matrix, while another part of the ZA is bonded to the glass surface. Finally, considering the in vitro results and our proposed model, the ratio between “free” and “bonded” ZA in our drug delivery systems showed in vitro evidence of a cancer treatment that selectively kills osteosarcoma cells while still favoring an osteogenic microenvironment. By overcoming the limitation of combining bisphosphonates with bioactive glasses, hydrogel-based drug delivery systems can be a solution for the development of new formulations proposed for bone cancer treatment in conjunction with bone regeneration.

Contemporary Review on Solubility Enhancement Techniques

The limited water solubility of pharmacoactive molecules hinders their ability to be used as pharmacological agents, yet the indispensability of a certain solubility parameter precludes any compromises. To overcome this challenge, various methods are employed in order to increase their bioavailability. Pharmaceutical molecules with lower solubility present an elevated risk of failure for drug development and innovation. Their solubility affects important processes such as pharmacokinetics, pharmacodynamics, distribution, protein binding, and absorption. As a result these parameters are greatly impacted by the dissolution rate of a particular molecule. Out of all pharmaceutical dosage forms, more than half are oral. For the drug molecule to reach its target site and be effective therapeutically, solubility and bioavailability must be taken into consideration. Unfortunately, during screening programs conducted by the pharmaceutical industry it became evident that nearly 40% of new chemical entities (NCEs) face various roadblocks when transitioning from formulation to development due to their poor solubility and bioavailability. The pharmaceutical industry is constantly confronted with the difficulty of improving drug bioavailability and solubility in formulations. This article covers a range of technological advancements to boost the solubility of insoluble drugs, such as complexation, emulsions and micelles production, microemulsion generation with cosolvents, polymeric micelle preparation methods, particle size decrease techniques, pharmaceutical salts application, prodrugs usage, solid-state alteration practices, soft gel technology implementation crystal engineering approaches and nanomorphology. Through this review, we will discuss a variety of more complex methods for improving solubility and bioavailability such as crystal engineering, micronization, solid dispersions, nano sizing, and use of cyclodextrins, solid lipid nanoparticles (SLNPs), colloidal drug delivery systems and drug conjugates. We'll also provide references to studies that have been conducted in connection with these topics.
 Keywords: Solubility, permeability, bioavailability, nano particles drug delivery systems, microemulsions, low water solubility

A SWOT analysis of nano co-crystals in drug delivery: present outlook and future perspectives.

The formulation of poorly soluble drugs is an intractable challenge in the field of drug design, development and delivery. This is particularly problematic for molecules that exhibit poor solubility in both organic and aqueous media. Usually, this is difficult to resolve using conventional formulation strategies and has resulted in many potential drug candidates not progressing beyond early stage development. Furthermore, some drug candidates are abandoned due to toxicity or have an undesirable biopharmaceutical profile. In many instances drug candidates do not exhibit desirable processing characteristics to be manufactured at scale. Nanocrystals and co-crystals, are progressive approaches in crystal engineering that can solve some of these limitations. While these techniques are relatively facile, they also require optimisation. Combining crystallography with nanoscience can yield nano co-crystals that feature the benefits of both fields, resulting in additive or synergistic effects to drug discovery and development. Nano co-crystals as drug delivery systems can potentially improve drug bioavailability and reduce the side-effects and pill burden of many drug candidates that require chronic dosing as part of treatment regimens. In addition, nano co-crystals are carrier-free colloidal drug delivery systems with particle sizes ranging between 100 and 1000 nm comprising a drug molecule, a co-former and a viable drug delivery strategy for poorly soluble drugs. They are simple to prepare and have broad applicability. In this article, the strengths, weaknesses, opportunities and threats to the use of nano co-crystals are reviewed and a concise incursion into the salient aspects of nano co-crystals is undertaken.

Formulation, Optimization and Characterization of Bupropion Hydrochloride Loaded Nanostructured Lipid Carriers for Intra-Nasal Administration: An Approach to Management of Smoking Cessation

Background: Tobacco smoking is a major factor leading to cardiovascular diseases. About 48% of cardiovascular diseases occur due to cigarette smoking. Bupropion hydrochloride is a non-nicotine treatment for smoking cessation. The existing marketed formulation of bupropion has limitations, like low bioavailability and extensive first-pass metabolism. In order to boost the bioa-vailability and increase the brain biodistribution of the drug, a colloidal drug delivery system, like nanostructured lipid carriers, is employed. Methods: NLC formulation was prepared using the microemulsion technique and an optimized formula was developed using a three-level factorial design. Results: The particle size of the optimized formulation was 162 nm, the polydispersity index was 12.2%, and the zeta potential was -29.0mV. Entrapment efficiency was found to be 41.2%. SEM images show that these NLCs are spherical. In vitro drug release study was conducted, and at the end of 72 hours, 50% of the drug was released, indicating the sustained release of the drug. Histo-pathological studies were conducted using goat nasal mucosa, and results indicated the NLC formu-lation as non-toxic for intranasal administration. Conclusion: Thus, through the intra-nasal route, an increased concentration of drug can be deliv-ered to the brain via the olfactory pathway, thereby improving the therapeutic effect and exhibiting better patient compliance in smoking cessation.

Risk-Assessment-Based Optimization Favours the Development of Albumin Nanoparticles with Proper Characteristics Prior to Drug Loading.

Albumin nanocarrier research and development is a challenging area in the field of personalized medicine and in providing advanced therapeutic solutions. Albumin as a biocompatible, nonimmunogenic, and non-toxic protein carrier that can be exploited to conjugate drugs with poor bioavailability to improve on this feature. With many different perspectives and desired target profiles, a systematic structural approach must be used in nanoparticle development. The extended Research and Development (R&D) Quality by Design thinking and methodology proved to be useful in case of specific nanoparticle development processes before. However, the coacervation method is the most frequently applied preparation method for HSA nanoparticles; there is a lack of existing research work which has directly determined the influence of process parameters, control strategy, or design space. With a quality-management-driven strategy, a knowledge space was developed for these versatile nanoparticles and an initial risk assessment was conducted on the quality-affecting factors regarding the coacervation method, followed by an optimization process via Plackett–Burman and Box–Behnken experimental design. As a result of screening the effect of process variables on the fabrication of HSA nanoparticles, an optimized colloidal drug delivery system was engineered with desired nanoparticulate properties.

An Overview of Nanostructured Lipid Carriers and its Application in Drug Delivery through Different Routes.

Nanostructured Lipid Carriers (NLC) are nano-sized colloidal drug delivery system that contains a lipid mixture consisting of both solid and liquid lipids in their core. This Lipid-Based Nanosystem is introduced as a biocompatible, non-toxic, and safe nano-drug delivery system as compared to polymeric or metallic nanoparticles. Due to its safety, stability, and high drug loading capacity compared to other lipid-based nanocarriers, NLC gained the attention of researchers to formulate safe and effective drug carriers. The ability to increase drug solubility and permeability while encapsulating the drug in a lipidic shell makes them an ideal carrier for drug delivery through difficult-to-achieve routes. Surface modification of NLC and the use of various additives result in drug targeting and increased residence time. With such qualities, NLCs can be used to treat a variety of diseases such as cancer, infections, neurodegenerative diseases, hypertension, diabetes, and pain management. This review focuses on the recent developments being made to deliver the drugs and genes through different routes via these nanocarriers. Here, we also discuss about historical background, structure, types of NLC and commonly employed techniques for manufacturing lipid-based nanocarriers.

Nanoarchitectonics of Layer-by-Layer (LbL) coated nanostructured lipid carriers (NLCs) for Enzyme-Triggered charge reversal

HypothesisCombined usage of Layer-by-Layer (LbL) coating and alkaline phosphatase (ALP) - responsive charge reversal strategies can improve the cellular internalisation of the colloidal drug delivery systems by also decreasing their cytotoxic effects. ExperimentsAnionic core NLCs were formed by combining the melt emulsification method and ultrasonication. The resulting core NLCs were coated sequentially first with protamine (Prot NLCs) and then with sodium tripolyphosphate (TPP) or sodium polyphosphate (Graham's salt, PP) generating TPP or PP NLCs, respectively. The developed NLCs were characterised regarding their size and zeta potential. Enzyme-induced charge reversal of the TPP and PP NLCs was evaluated by zeta potential measurements upon their incubation with alkaline phosphatase (ALP). In parallel, time-dependent phosphate release was monitored in the presence of isolated as well as cell-associated ALP. Morphological evaluations were performed by scanning electron microscopy (SEM) studies. Moreover, cell viability and cellular uptake studies were carried out in vitro on Caco-2 cells. FindingsThe core NLCs were obtained with a mean size of 272.27 ± 5.23 nm and a zeta potential of −25.70 ± 0.26 mV. Upon coating with protamine, the zeta potential raised to positive values with a total change up to Δ29.3 mV also displaying an increase in particle size. The second layer coating with TPP and PP provided a negative surface charge. Subsequent to ALP treatment, the zeta potential of the TPP and PP NLCs reversed from negative to positive values with total changes of Δ8.56 and Δ7.47 mV, respectively. Conformably, significant amounts of phosphate were released from both formulations. Compared with core NLCs, improved cellular viability as well as increased cellular uptake were observed in case of Prot, TPP and PP NLCs.

Biodegradable Polymers-Based Smart Nanocrystals for Loxoprofen Delivery with Enhanced Solubility: Design, Fabrication and Physical Characterizations.

Nanocrystals are carrier-free, submicron-sized, colloidal drug delivery systems with particle sizes in the mean nanometer range. Nanocrystals have high bioavailability and fast absorption because of their high dissolution velocity and enhanced adhesiveness to cell membranes. Loxoprofen, a nonsteroidal anti-inflammatory drug belonging to the Biopharmaceutical Classification System (BCS) II drug class, was selected as the model drug. The aim of this study was to formulate nanocrystals of loxoprofen. A total of 12 formulations (F1 to F12) were prepared. An antisolvent technique was used to determine the effects of various stabilizers and processing conditions on the optimization of formulations. The various stabilizers used were hydroxypropyl methylcellulose (0.5%), polyvinylpyrrolidone (0.5%), and sodium lauryl sulfate (0.1%). The various characterizations conducted for this research included stability studies at 25 °C and 4 °C, scanning electron microscopy, transmission electron microscopy (TEM), X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC), zeta potentials, polydispersity indexes, and dissolution studies. F10 was the optimized formulation that showed stability at room temperature, as well as at a refrigerated temperature, for 30 days. A high dissolution rate (100% within the first 10 min) was shown by comparative dissolution studies of nano-suspensions with the micro-suspension and raw loxoprofen. F10 formulation had a non-porous and crystalline morphology on evaluation by TEM and XRPD, respectively, and the average particle size was 300 ± 0.3 nm as confirmed by TEM. DSC recorded a reduction in the melting point (180 °C processed and 200 °C unprocessed melting points). The dissolution rate and solubility of the formulated loxoprofen nanocrystals were significantly enhanced. It can be concluded that selecting suitable stabilizers (i.e., polymers and surfactants) can produce stable nanocrystals, and this can potentially lead to a scaling up of the process for commercialization.

Bioavailability Enhancement Techniques for Poorly Aqueous Soluble Drugs and Therapeutics.

The low water solubility of pharmacoactive molecules limits their pharmacological potential, but the solubility parameter cannot compromise, and so different approaches are employed to enhance their bioavailability. Pharmaceutically active molecules with low solubility convey a higher risk of failure for drug innovation and development. Pharmacokinetics, pharmacodynamics, and several other parameters, such as drug distribution, protein binding and absorption, are majorly affected by their solubility. Among all pharmaceutical dosage forms, oral dosage forms cover more than 50%, and the drug molecule should be water-soluble. For good therapeutic activity by the drug molecule on the target site, solubility and bioavailability are crucial factors. The pharmaceutical industry’s screening programs identified that around 40% of new chemical entities (NCEs) face various difficulties at the formulation and development stages. These pharmaceuticals demonstrate less solubility and bioavailability. Enhancement of the bioavailability and solubility of drugs is a significant challenge in the area of pharmaceutical formulations. According to the Classification of Biopharmaceutics, Class II and IV drugs (APIs) exhibit poor solubility, lower bioavailability, and less dissolution. Various technologies are discussed in this article to improve the solubility of poorly water-soluble drugs, for example, the complexation of active molecules, the utilization of emulsion formation, micelles, microemulsions, cosolvents, polymeric micelle preparation, particle size reduction technologies, pharmaceutical salts, prodrugs, the solid-state alternation technique, soft gel technology, drug nanocrystals, solid dispersion methods, crystal engineering techniques and nanomorph technology. This review mainly describes several other advanced methodologies for solubility and bioavailability enhancement, such as crystal engineering, micronization, solid dispersions, nano sizing, the use of cyclodextrins, solid lipid nanoparticles, colloidal drug delivery systems and drug conjugates, referring to a number of appropriate research reports.

Rhodojaponin III-Loaded Chitosan Derivatives-Modified Solid Lipid Nanoparticles for Multimodal Antinociceptive Effects in vivo.

BackgroundRhodojaponin III (RJ-III) is a bioactive diterpenoid, which is mainly found in Rhododendron molle G. Don (Ericaceae), a potent analgesia in traditional Chinese medicine with several years of clinical applications in the country. However, its clinical use is limited by its acute toxicity and poor pharmacokinetic profiles. To reduce such limitations, the current study incorporated RJ-III into the colloidal drug delivery system of hydroxypropyl trimethyl ammonium chloride chitosan (HACC)-modified solid lipid nanoparticles (SLNs) to improve its sustained release and antinociceptive effects in vivo for oral delivery.ResultsThe optimized RJ-III@HACC-SLNs were close to spherical, approximately 134 nm in size, and with a positive zeta potential. In vitro experiments showed that RJ-III@HACC-SLNs were stable in the simulated gastric fluid and had a prolonged release in PBS (pH = 6.8). Pharmacokinetic results showed that after intragastric administration in mice, the relative bioavailability of RJ-III@HACC-SLNs was 87.9%. Further, it was evident that the peak time, half-time, and mean retention time of RJ-III@HACC-SLNs were improved than RJ-III after the administration. In addition, pharmacodynamic studies revealed that RJ-III@HACC-SLNs markedly reduced the acetic acid, hot, and formalin-induced nociceptive responses in mice (P < 0.001), and notably increased the analgesic time (P < 0.01). Moreover, RJ-III@HACC-SLNs not only showed good biocompatibility with Caco-2 cells in vitro but its LD50 value was also increased by 1.8-fold as compared with that of RJ-III in vivo.ConclusionThese results demonstrated that RJ-III@HACC-SLNs improved the pharmacokinetic characteristics of the RJ-III, thereby exhibiting toxicity-attenuating potential and antinociceptive enhancing properties. Consequently, HACC-SLNs loaded with RJ-III could become a promising oral formulation for pain management that deserves further investigation in the future.

Promising Strategies of Colloidal Drug Delivery-Based Approaches in Psoriasis Management.

Psoriasis is a chronic inflammatory autoimmune disorder that moderately affects social and interpersonal relationships. Conventional treatments for psoriasis have certain problems, such as poor drug penetration through the skin, hyper-pigmentation, and a burning sensation on normal and diseased skin. Colloidal drug delivery systems overcome the pitfalls of conventional approaches for psoriasis therapeutics and have improved patient safety parameters, compliance, and superior effectiveness. They also entail reduced toxicity. This comprehensive review’s topics include the pathogenesis of psoriasis, causes and types of psoriasis, conventional treatment alternatives for psoriasis, the need for colloidal drug delivery systems, and recent studies in colloidal drug delivery systems for the treatment of psoriasis. This review briefly describes colloidal drug delivery approaches, such as emulsion systems—i.e., multiple emulsion, microemulsion, and nano-emulsion; vesicular systems—i.e., liposomes, ethosomes, noisomes, and transferosomes; and particulate systems—i.e., solid lipid nanoparticles, solid lipid microparticles, nano-structured lipid carriers, dendrimers, nanocrystals, polymeric nanoparticles, and gold nanoparticles. The review was compiled through an extensive search of the literature through the PubMed, Google Scholar, and ScienceDirect databases. A survey of literature revealed seven formulations based upon emulsion systems, six vesicular drug delivery systems, and fourteen particulate systems reported for antipsoriatic drugs. Based on the literature studies of colloidal approaches for psoriasis management carried out in recent years, it has been concluded that colloidal pharmaceutical formulations could be investigated broadly and have a broad scope for effective management of many skin disorders in the coming decades.

Formulation and Characterization of Bitter Melon (Momordica charantia Linn.) Fruit Fraction Loaded Solid Lipid Nanoparticles

Background: The main active compound of bitter melon (Momordica charantia Linn.) fruit is charantin, which is believed to have important role on antihyperglycemic effect. However, charantin compound has a large molecular weight and is easily hydrolysed when given orally. Therefore, a colloidal drug delivery system, such as solid lipid nanoparticles (SLN), is required to provide a suitable and effective delivery of charantin, which is contained in a bitter melon fraction (BMF). Objective: This study aimed to prepare and evaluate SLN containing BMF with an appropriate characteristic for transdermal delivery. Methods: Bitter melon fruits were extracted with ionic liquid of [BMIM]BF4 using ultrasound-assisted extraction (UAE) and fractionated with dichloromethane. Four formulas of BMF loaded SLN were prepared with various ratio of BMF to surfactant and various ratio of lipids using high-shear homogenization followed by ultrasonication method. The obtained SLN were characterized, including morphology, particle size distribution, zeta potential, and entrapment efficiency. Furthermore, the stability study of BMF-loaded SLN was also conducted. Results: The result showed that BMF was a dry powder and brownish fraction with a specific smell. The BMF loaded SLN showed a spherical shape with the SLN F1 formula as a selected formula. The SLN F1 showed a particle size (Z-average) of 98.3±1.98 nm, polydispersity index of 0.26±0.01, zeta potential of -39.53±0.15 mV, and entrapment efficiency of 82.96±1.42 %. According to the stability study, it revealed that the BMF loaded SLN F1 had an acceptable stability, which the charantin content in the SLN was 96.52% after 3 months storage at 25°C ± 2°C. Conclusion: The BMF loaded SLN F1 with 1:12 ratio of BMF to surfactant and 1:2 ratio of capric caprylic triglyceride to glyceryl monostearate was selected as the best formula with the appropriate characteristics for transdermal delivery.

Thymol and Piperine-Loaded Poly(D,L-lactic-co-glycolic acid) Nanoparticles Modulate Inflammatory Mediators and Apoptosis in Murine Macrophages

AbstractThis study aimed at preparing and characterizing thymol, eugenol, and piperine-loaded poly(D,L-lactic-co-glycolic acid) nanoparticles and evaluating the effect on inflammatory mediators secretion and apoptosis in Raw 264.7 macrophage cells. Nanoparticles were produced by the solvent evaporation technique. Dynamic light scattering and scanning electron microscopy were used to study the physicochemical characteristics. Raw 264.7 macrophage cells were used as a model for in vitro assays. The 2-(4-iodophenyl)-3-(4-nitrophenyl)-5-(2,4-disulfophenyl)-2H-tetrazolium assay was used to determine the cytotoxicity of the formulated nanoparticles. An annexin V apoptosis detection kit was used to assess apoptosis. Nitric oxide production was determined using the Griess reagent, and the inflammatory mediators level was evaluated with Th1/Th2 cytokine and fluorometric cyclooxygenase kits. The loaded nanoparticles showed a particle size around 190 nm with a low polydispersity between 0.069 and 0.104 and a zeta potential between–1.2 and–9.5 mV. Reduced cytotoxicity of nanoparticles compared to free molecules against Raw 264.7 macrophage cells was observed and seemed to occur through a mechanism associated with apoptosis. A decrease in cyclooxygenase enzyme activity with an increasing concentration was observed. Both free molecules and nanoparticles showed their capacity to modulate the inflammatory process mostly by inhibiting the investigated inflammatory cytokines. The data presented in this study indicate that thymol and piperine-loaded poly(D,L-lactic-co-glycolic acid nanoparticles could serve as a novel anti-inflammatory colloidal drug delivery system with reduced toxicity. However, further study should be considered to optimize the formulation’s loading capacity and thereby probably enhance their bioactivity in treating inflammatory diseases.

Lipid-Based Drug Delivery Systems in Regenerative Medicine.

The most important goal of regenerative medicine is to repair, restore, and regenerate tissues and organs that have been damaged as a result of an injury, congenital defect or disease, as well as reversing the aging process of the body by utilizing its natural healing potential. Regenerative medicine utilizes products of cell therapy, as well as biomedical or tissue engineering, and is a huge field for development. In regenerative medicine, stem cells and growth factor are mainly used; thus, innovative drug delivery technologies are being studied for improved delivery. Drug delivery systems offer the protection of therapeutic proteins and peptides against proteolytic degradation where controlled delivery is achievable. Similarly, the delivery systems in combination with stem cells offer improvement of cell survival, differentiation, and engraftment. The present review summarizes the significance of biomaterials in tissue engineering and the importance of colloidal drug delivery systems in providing cells with a local environment that enables them to proliferate and differentiate efficiently, resulting in successful tissue regeneration.