Preparation Of Nanostructured Lipid Carriers Research Articles

Ibrutinib topical delivery for melanoma treatment: The effect of nanostructured lipid carriers’ composition on the controlled drug skin deposition

Melanoma is responsible for more than 80% of deaths related to skin diseases. Ibrutinib (IBR), a Bruton's tyrosine kinase inhibitor, has been proposed to treat this type of tumor. However, its low solubility, extensive first-pass effect, and severe adverse reactions with systemic administration affect therapeutic success. This study proposes developing and comparing the performance of two compositions of nanostructured lipid carriers (NLCs) to load IBR for the topical management of melanomas in their early stages. Initially, the effectiveness of IBR on melanoma proliferation was evaluated in vitro, and the results confirmed that the drug reduces the viability of human melanoma cells by inducing apoptosis at a dose that does not compromise dermal cells. Preformulation tests were then conducted to characterize the physical compatibility between the drug and the selected components used in NLCs preparation. Sequentially, two lipid compositions were used to develop the NLCs. Formulations were then characterized and subjected to in vitro release and permeation tests on porcine skin. The NLCs containing oleic acid effectively controlled IBR release over 24 h compared to the NLCs composed of pomegranate seed oil. Furthermore, the nanoparticles acted as permeation enhancers, increasing the fluidity of the lipids in the stratum corneum, as determined by EPR spectroscopy, which stimulated the IBR penetration more profoundly into the skin. However, the NLCs composition also influenced the permeation promotion factor. Thus, these findings emphasize the importance of the composition of NLCs in controlling and increasing the skin penetration of IBR and pave the way for future advances in melanoma therapy.

Nanostructured Lipid Carrier for Hyperpigmentation Treatment - a Dermal Prospective

The normal human skin is exposed to different types of infection like wrinkles, pigmentation, acne, pimples in which pigmentation is most common in women over 30-40 years. The field of nanotechnology is currently intensely exploited for drug delivery technology for passive and active targeting via various routes of administration, such things can be effectively treated by incorporating the drug, loaded in a Nanostructured lipid carrier (NLC). NLCs have shown potential in delivering poorly soluble active components and in depigmenting. NLC springs up as the second generation of lipid nanoparticles to overcome the shortcomings of first generation through the topical route. NLC in topical administration provides some added advantages like increasing skin hydration and modified release profile and increase in skin penetration leading to avoidance of systemic absorption. NLCs are composed of biocompatible lipids, surfactants, and cosurfactants which help enhance drug loading capacity and stabilize the formulation. NLC's remarkable physicochemical and subsequently biocompatible qualities have created an ongoing need for the development of beneficial and safe drug delivery methods. The key attributes of NLC that make them a promising drug delivery system are ease of preparation, biocompatibility, the feasibility of scale-up, non-toxicity, improved drug loading, and stability Their ingredients have a special impact on the end product's physicochemical characteristics and efficacy. The present review aims to focus on the recent advancement in the preparation, characterization, and applications of NLC in treating hyperpigmentation.

Screening and selection of formulation components of nanostructured lipid carriers system for Mitragyna Speciosa (Korth). Havil drug delivery

Nanostructured lipid carriers (NLC) have evolved as effective vehicles for improving the bioavailability of poorly water-soluble drugs as well as protecting them from degradation and metabolism. The present study investigated the preformulation and its impact on different liquid lipids and solid lipids with diverse chemical structures and hydrophilic-lipophilic balance (HLB) for the critical quality attributes of Mitragyna speciosa leaves extract (MS)-based nanostructured lipid carriers suitable for drug delivery system. The presence of bioactive alkaloids (mitragynine, 7-hydroxymitragynine, speciogynine), flavonoids (quercetin, apigenin, kaempferol), saponins (daucosterol, quinovic acid 3-o-beta-d-quinovopyranoside, 1-o-feruloyl-beta-d-glucose), and other bioactive phytochemicals (chlorogenic acid, umbelliferone, ursolic acid) in MS leaves extract was detected using LCMS/MS analysis to support its medicinal properties. The total phenolic content, total flavonoid content, and DPPH assay of MS were 90.88 ± 0.30 GAE mg/g, 50.43 ± 0.47 QE mg/g, and IC50 at 0.0397 ± 0.0035 mg/mL, respectively. The screening preparation of NLC requires the selection of liquid lipid (oil), solid lipid, and surfactant. Based on the solubility test, the maximum solubility of MS leaves extract in oleic acid (liquid lipid) and compritol ATO 888 (solid lipid) were 2.859 ± 0.010% and 53.02 ± 0.39% respectively at ratio 70:30. Tween 80 was selected as the main surfactant for the preparation of NLC due to its highest emulsification efficiency (51.53%). The antimicrobial study showed that MS leaves extract gives antimicrobial effect towards Streptococcus aureus bacteria. The preformulation information collected offers a better, efficient, and cost-effective choice for further formulation development of MS leaves extract in drug delivery systems.

Nanostructured Lipid Carriers: A Promising Carrier in Targeted Drug Delivery System

Abstract: Nanostructured lipid carriers (NLCs) are considered second-generation lipid-based pharmaceutical formulations in drug delivery systems. It is a more efficient drug delivery system that includes the development of a nano-particulate system, and it is superior to the conventional drug delivery system. Among all available nanoparticles, NLC has gained more attention due to its superior characteristics, such as being lipophilic, biodegradable, and biocompatible. This lipid nanoparticulate system is more advantageous over liposomes, microparticles, emulsions, and solid lipid nanoparticles. NLCs have emerged as a promising carrier for the delivery of targeted drug substances via oral, parenteral, topical, pulmonary, transdermal, and ocular routes. These nanocarriers are utilized for the delivery of both lipophilic as well as hydrophilic drugs. NLCs are composed of a matrix of physiological lipids, i.e., solid lipid and liquid lipid, emulsifiers, and water. NLCs provide an opportunity for large-scale production, ease of preparation with enhanced encapsulation, targeted efficiency, and reduced toxic effects. This review is focused on the advantages, limitations, methods of preparation, characterization, and applications of NLCs.

Impact of Parameter on Nanostructured Lipid Carrier Formulation and Approach of the Carrier for Cancer Treatment: a Brief Study

Introduction. For the last decade, nanotechnology has been studied extensively in the pharmaceutical field. Among all the nanotechnology formulation areas, nanostructured lipid carrier is enormously researched by formulation scientists as it is one of the focused areas of lipid carrier for the effective formulation.Materials and methods. The nanostructured lipid carrier (NLC) consists of solid lipid, liquid lipid & surfactant for fabrication of formulation. Methods such as high energy methods, low energy methods and organic solvent-based methods are used for the preparation of NLC. As per literature study the High pressure homogenization is the most efficient method for fabrication of formulation.Results and discussion. This carrier system has significant advantages such as high drug entrapment, improved bioavailability, stability during storage, and targeting the site with a better-controlled release making it a prominent area for the formulator to emphasize on it. Although many drugs are formulated with a nanostructured lipid carrier, it is a concern for researchers to find out the effectiveness of formulation by studying the process parameter and safety.Conclusion. The present review was focused to study the impact of various parameters such as Lipid, surfactant, homogenization rate, preservative, Crystallinity, and surface charge on the formulation. The study also extended towards toxicity and biocompatibility, topical targeting & cancer treatment of the Nanostructured lipid carrier.

Microneedle mediated transdermal delivery of β-sitosterol loaded nanostructured lipid nanoparticles for androgenic alopecia

Plant-derived 5 α-reductase inhibitors, such as β-sitosterol and phytosterol glycosides, have been used to treat androgenic alopecia, but their oral absolute bioavailability is poor. This study aimed to develop a transdermal drug delivery system of β-sitosterol (BS) using a nanostructured lipid carrier (NLC) incorporated into polymeric microneedles (MN). Using a high-speed homogenization method, NLC was formulated variables were optimized by Box-Behnken statistical design. The optimized formulation of BS-loaded NLCs was incorporated into the chitosan-based MNs to prepare NLC-loaded polymeric MNs (NLC-MNs) and evaluated using testosterone induced alopecia rats. The cumulative amount of β-sitosterol associated with NLC- MN which penetrated the rat skin in-vitro was 3612.27 ± 120.81 μg/cm2, while from the NLC preparation was 2402.35 ± 162.5 μg/cm2. The steady state flux (Jss) of NLC-MN was significantly higher than that of the optimized NLC formulation (P < 0.05). Anagen/telogen ratio was significantly affected by NLC and NLC-MN, which was 2.22 ± 0.34, 1.24 ± 0.18 respectively compared to 0.26 ± 0.08 for animal group treated with testosterone. The reversal of androgen-induced hair loss in animals treated with β-sitosterol was a sign of hair follicle dominance in the anagenic growth phase. However, NLC–MN delivery system has shown significant enhancement of hair growth in rats. From these experimental data, it can be concluded that NLC incorporated MN transdermal system have potential in effective treatment of androgenic alopecia.

Nanostructured Lipid Carriers: A Vital Drug Carrier for Migraine Treatment

Migraine is a very mysterious and much-misunderstood disorder characterized by pulsating headache in one side of the head in the form of attacks lasting from 4-48 hrs. It is a complex neurological condition, in this condition which can affect the whole body with many symptoms. However to cure this and effective treatment the nanostructured lipid carriers are used as widely nowadays. This use of structures ranges from the size 1-100nm with the main aim to develop the medicine to diagnose as accurately and effectively with less or no side effects. As we developed the stability and leakage of drugs is also improved. As we know the limitations from the different routes of administration are first-pass metabolism, poor bioavailability, and poor solvency to overcome these limitations Nanostructured lipid carriers (NLCs) were prepared. Transdermals, ocular, oral, topical, and parenteral are the different routes through which Nano based systems are delivered. Spatially incompatible liquid lipids and solid lipids are blended and NLCs were prepared. The main advantages of drug therapy over conventional carriers NLCs are improved bioavailability, increased solubility. This review describes the NLC used for the migraine treatments, its advantages, and disadvantages, types, NLC techniques, mode of action, of NLC. Imperfect, amorphous, and multiple types are the main three types of NLCs. Lipids like solid and liquid, Emulsifiers, and aqueous medium were the excipients used. Micro-emulsion technique, micro-emulsion-based SLN/NLC preparations, solvent diffusion method, high-pressure homogenization (HPH), hot and cold homogenization techniques, and melt emulsification method are the techniques used for the preparation of NLC.

Design, optimization and in-vivo characterization of mupirocin loaded nanostructured lipid carrier based gel for effective treatment of impetigo

Mupirocin is a broad-spectrum antibiotic effective in treatment of skin infection (Impetigo), but the poor bioavailability limits its use as a conventional dosage form such as tablets, ointment and cream. The present investigation was aimed to design, optimize and evaluate Mupirocin (MC) loaded nanostructured lipid carriers (NLCs) based gel for topical application. Excipients identified were screened for apposite material required for the formulation of NLCs using process variables as the determining factors. The preparation of nanostructured lipid carriers (NLCs) was optimized using 32 factorial design with two independent variables (solid: liquid lipid ratio and surfactant (%)) and two responses (particle size (nm), entrapment efficiency (%)) using hot high pressure homogenization method. The formulation was further characterized for zeta potential (mV), polydispersity index and morphology. The optimized NLC dispersion of Mupirocin (MC) was lyophilized and loaded in 0.75% w/v Carbopol 980 gel and was evaluated for pH, viscosity and drug content. Mupirocin (MC) loaded NLC based gel were characterized for ex-vivo drug permeation and compared with marketed (cream) preparation. Further, drug deposition, skin irritation and stability study was carried out as per ICH guidelines. The optimized formulation (F5) containing Glyceryl behenate: Oleic acid (70:30), and Poloxamer 188 (0.5%) demonstrated smaller particle size (150.02 ± 1.52 nm) with higher drug entrapment efficiency (88.02 ± 1.21%). Mupirocin (MC) loaded NLC based gel demonstrated sustained drug profile with significant increase (P < 0.05) in drug deposition in skin (about 26%) with non-irritant properties to the skin. Stability study showed no significant changes of the parameters during and after the study. In conclusion, developed Mupirocin (MC) loaded NLC based gel could serve as a novel approach in treatment of impetigo by deliver the drug topically with sustained effect and improved patient compliance.

Olanzapine Loaded Nanostructured Lipid Carriers via High Shear Homogenization and Ultrasonication

The aim of this study was to understand the effect of high shear homogenization (HSH) and ultrasonication (US) on the physicochemical properties of blank and olanzapine loaded nanostructured lipid carriers (NLCs) along with their drug loading potential and drug release profiles from formulated particles. NLCs were prepared with different ratios of Compritol and Miglyol as the solid and liquid lipids, respectively, under changing HSH and US times between 0 to 15 min. The surfactants (Poloxamer 188 (P188) and tween 80) and the drug content was kept constant in all formulations. The prepared NLCs were evaluated for particle size, polydispersity index, zeta potential, drug crystallinity and chemical interactions between lipids and OLZ. The in-vitro drug release was performed using dialysis tube method in phosphate buffer solution (PBS) at pH 7.4. The formulated NLCs were negatively charged, spherically shaped and monodisperse, with particle sizes ranging from 112 to 191 nm. There was a significant influence of US time on the preparation of NLCs in comparison to HSH, where a significant reduction in the mean particle diameter was seen after 5 min of sonication. An increase of Miglyol content in NLCs led to an increase in particle size. In general, application of US led to decrease in particle size after HSH but an increase in particle diameter of low Miglyol containing preparation was also observed with longer sonication time. OLZ was successfully encapsulated in the NLCs and a total release of 89% was achieved in 24 h in PBS at pH 7.4.

Methods for preparation of nanostructured lipid carriers.

Construction of nanocarriers of different structures and properties have shown great promise as delivery systems for a wide range of drugs to improve therapeutic effects and reduce side effects. Nanostructured lipid carriers (NLCs) have been introduced as a new generation of solid lipid nanoparticles (SLNs) to overcome several of the limitations associated with the SLNs. NLCs consist of a blend of solid and liquid lipids which result in a partially crystallized lipid system that enables higher drug loading efficiency compared to SLNs. Owing to their biocompatibility, low toxicity, ease of preparation and scaling-up, and high stability, NLCs have been exploited in numerous pharmaceutical applications. Different methods for fabrication of NLCs have been described in the literature. In this article, procedures involved in emulsification-solvent evaporation method, one of the commonly utilized methods for preparation of NLCs, are described in detail. Critical aspects that should be considered throughout preparation process are also highlighted to allow for consistent and reproducible construction of NLCs.

Preformulation and characterization of raloxifene-loaded lipid nanoparticles for transdermal administration.

Transdermal administration of raloxifene hydrochloride (RLX)-loaded nanostructured lipid carriers (NLCs) has been proposed to circumvent its low oral bioavailability (2%). Preformulation studies were carried out to evaluate drug-excipient compatibility of various adjuvants commonly used for NLC preparation (waxes, cholesterol, compritol, gelucire, span 60, span 80, span 85, tween 80, poloxamer 188, oleic acid, caprylic/capric triglyceride, and castor oil). It was used differential scanning calorimetry (DSC), isothermal stress testing (IST), and solubility studies. The most promising excipients were chosen for NLC obtention, and full characterization was done, including in vitro skin permeation. DSC curves suggested drug-excipient interaction among some compounds, and the IST study showed incompatibility of RLX with waxes, compritol, cholesterol, span 60, and poloxamer 188. Solubility studies helped select gelucire, caprylic/capric triglyceride, span 80, and tween 80 for NLC production. Twelve NLCs were obtained (NLC1 to NLC12), but NLC7 and NLC8 were the most promising ones. In vitro release studies demonstrated that NLC7 and NLC8 were able to control RLX release (14.74 and 9.07% at 24h, respectively) compared with the unloaded drug (> 90% at 24h). Unloaded RLX did not permeate the diffusion cells' receptor medium and showed higher drug skin retention (11-fold) than RLX-loaded NLC. NLC reduced RLX skin retention, favoring drug permeation to deeper skin layers. NLC7 increased drug flux is 2.4-fold. NLC7 is a promising formulation for RLX transdermal drug delivery.

Design and Optimization of Febuxostat-loaded Nano Lipid Carriers Using Full Factorial Design.

This work aims to develop nanostructured lipid carriers (NLCs) to improve the oral bioavailability of febuxostat (FEB). High shear homogenization, a well-known technique, followed by bath sonication with slight modifications was used to prepare FEB-loaded NLCs using oleic acid as liquid lipid and stearic acid as solid lipid. A total of 3² full factorial design was utilized to examine the effect of 2 independent variables, namely, X1 (liquid to solid lipid ratio) and X2 (surfactant concentration) on the Y1 (particle size) and Y2 (% entrapment efficiency) of the drug. The prepared NLCs were evaluated for particle size, polydispersity index, zeta potential, and (%) entrapment efficiency. The drug's highest solubility was found in the stearic (solid lipid) and oleic acid (liquid lipid), which were further chosen for NLC preparation. Result of the present study showed an increase in entrapment efficiency and a decrease in particle size with the increase in liquid lipid to solid lipid ratio. With increased surfactant concentration, a small particle size is observed. The optimized formulation's particle size and (%) entrapment efficiency was found to be 99 nm and 80%, respectively. The formulations' zeta potential and polydispersity index were found within the range. Compared to plain drug suspension, the optimized formulation showed higher drug release, which may be due to the presence of the higher amount of liquid lipid. The particles shown in the transmission electron microscopy were round in shape and have smooth surface. Stability studies showed that the NLC formulation can be stored for a longer time period under room condition. FEB-loaded NLC were successfully prepared using full 3² factorial design, and can be further used for oral delivery of FEB for gout treatment.

An Overview of Second Generation Nanoparticles− Nanostructure Lipid Carrier Drug Delivery System

Lipids are used as vehicles for the preparation of various formulations prescribed for administrations, including emulsions, ointments, suspension, tablets, and suppositories. The first parental nano-emulsion was discovered from the 1950s when it was added to the intravenous administration of lipid and lipid-soluble substances. Lipid-based drug delivery systems are important nowadays. Solid nanoparticles (SLN) and Nanostructured lipid carriers (NLC) are very proficient due to the ease of production process, scale-up capability, bio-compatibility, the biodegradability of formulation components and other specific features of the proposed route. The administration or nature of the materials must be loaded into these delivery systems. The main objectives of this review are to discuss an overview of second-generation nanoparticles, their limitations, structures, and route of administration, with emphasis on the effectiveness of such formulations. NLC is the second generation of lipid nanoparticles having a structure like nanoemulsion. The first generation of nanoparticles was SLN. The difference between both of them is at its core. Both of them are a colloidal carrier in submicron size in the range of 40-1000 nm. NLC is the most promising novel drug delivery system over the SLN due to solving the problem of drug loading and drug crystallinity. Solid and liquid lipids combination in NLC formation, improve its quality as compare to SLN. NLC has three types of structures: random, amorphous, and multiple. The random structure containing solid-liquid lipids and consisting crystal and the liquid lipid irregular in shape; thereby enhance the ability of the lipid layer to pass through the membrane. The second is the amorphous structure. It is less crystalline in nature and can prevent the leakage of the loaded drug. The third type is multiple structures, which have higher liquid lipid concentrations than other types. The excipients used to form the NLC are bio-compatible, biodegradable and non-irritating, most of which can be detected using GRAS. NLC is a promising delivery system to deliver the drug through pulmonary, ocular, CNS, and oral route of administration. Various methods of preparation and composition of NLC influence its stability Parameters. In recent years at the educational level, the potential of NLC as a delivery mechanism targeting various organs has been investigated in detail.

Preparation of 9Z-β-Carotene and 9Z-β-Carotene High-Loaded Nanostructured Lipid Carriers: Characterization and Storage Stability.

Cis (Z)-β-carotenes with 25.3% 9Z-β-carotene were prepared for nanostructured lipid carriers (NLCs). The optimal conditions for NLC preparation using an orthogonal experimental method were as follows: the total lipid concentration was 9% (w/v), the surfactant concentration was 1.4% (w/v), the solid to liquid lipid ratio was 3:1 (w/w), and the homogenization pressure was set at 500 bar for three cycles. Under these conditions, the encapsulation efficiency (%) of the NLC was 95.64%, and the total β-carotene in NLCs was 2.9 mg/mL, which was significantly higher than those reported by others. The proportion of total Z-β-carotenes was as high as 53.3%, the particle size was 191 ± 6.46 nm, and the polydispersity index was 0.2 ± 0.03. Storage stability results indicated that the β-carotene-loaded NLC stabilizes both 9Z-β-carotene and total β-carotene from leakage and degradation during 21 days of storage at pH 3.5-7.5 at low temperatures (4 °C), especially for the more bioactive 9Z-β-carotene. The technique with an improved ratio of 9Z-β-carotene, loading capacity, water solubility, and bioaccessibility of the β-carotene NLC provides an effective strategy for β-carotene applications in functional foods or beverages and in nutraceutical preparations.

CUSTOM DESIGN PERSPECTIVE IN THE PROCESS PARAMETER OPTIMIZATION OF NANO LIPID CARRIERS

Objective: Nanostructured lipid carrier is an emerging lipid-derived delivery system that is rapidly gaining popularity due to the simplicity of the manufacturing technique. The primary task in formulating nanoparticles is to optimize the parameters that are involved in the process. The rationale behind this study is to optimize the process parameters for the preparation of nanostructured lipid carriers. &#x0D; Methods: The optimization of selected techniques hot homogenization with ultra-sonication and melt dispersion technique, was carried out via statistical analysis software JMP version 13 Pro using custom design approaches. Sonication time, homogenization speed, stirring rate, and cooling temperature were selected as factors for hot homogenization. Stirring speed, stirring time, and dilution volume were the factors deliberated for melt dispersion. The impact of these factors on the responses, particle size, and polydispersity index were studied. The nanoparticles were prepared according to the ten experimental runs generated by the design. Based on the responses, the design space and optimum framework were selected. &#x0D; Results: The prediction profiler indicated maximum desirability at 81% and 80% for hot homogenization and melt dispersion respectively. The actual versus predicted plot of particle size indicated a regression coefficient (R2) of 0.98, and a p-value of 0.0001 for hot homogenization and for melt dispersion the corresponding values were 0.95 and 0.0003. For the response polydispersity index, these values were 0.92 and 0.0052 for hot homogenization and 0.90 and 0.0024 for melt dispersion.&#x0D; Conclusion: The endorsing results indicated the authenticity of the model in predicting the significant processing parameters for NLC.

Types of Solid Lipids on Physical Stability of Resveratrol-Loaded Nanostructured Lipid Carriers

Resveratrol (Res) loaded nanostructured lipid carriers (NLCs) were prepared by high shear homogenization and ultrasonication technique. Caprylic/capric glyceride (IM) was used as a liquid lipid, while glyceryl monostearate (GMS), beeswax (BW), palmitic acid (PA) and myristic acid (MA) at various concentrations (5, 10, 15, and 20 %w/w) were solid lipids. Polyoxyethylene 20 sorbitan monooleate or polysorbate 80 (Tween® 80) was use as a surfactant. The results showed that all concentration of PA and MA can be prepared the smaller particle NLC than that using GMS and BW according to the small molecule of MA and PA. The zeta potential of Res loaded NLCs were negative charge (-24.30 to -37.80 mV), which could be considered as a stable system. The stability studies revealed that NLCs with MA and PA showed a - high stability in particle size and zeta potential after storage at 40 ± 2°C /75 %RH for 3 months. These results suggested the MA and PA were suitable solid lipids for the NLCs preparation which have potential to be a nanoparticulate carrier for Res delivery.

Improved anti-arthritic activity of ginger extract, a traditional medicine, using novel drug delivery approach.

Ginger and castor oil, both are used in traditional medicine to treat arthritis, the latter is also commonly used as a vehicle in these systems of medicine. The study was designed to prepare a nanostructured lipid carrier (NLC) of ginger extract using castor oil as a novel liquid lipid and evaluate its safety and efficacy in rheumatoid arthritis in experimental animals. Ginger extract was standardized using High performance liquid chromatography (HPLC). The optimized NLC formulation was characterized and its therapeutic efficacy was evaluated in Chronic Freund's adjuvant (CFA) induced arthritis in experimental animals. Ginger extract contained 38.76±3.01%w/w of 6-gingerol. The optimized NLC formulation showed a particle size of around 205nm, a zeta potential of-33.7 and %entrapment efficiency of 76.59±0.83%. Reduction in primary inflammation was significantly higher with NLC when compared with ginger extract and castor oil alone (p<0.001). The formulation also improved hyperalgesia in rats. Castor oil can be used as a novel lipid in the preparation of NLC. The NLC effectively enhanced the therapeutic value of poorly bioavailable ginger extract.

Nanostructured Lipid Carriers (NLCs) for Drug Delivery: Role of Liquid Lipid (Oil).

In recent years, SLNs and NLCs are among the popular drug delivery systems studied for the delivery of lipophilic drugs. Both systems have demonstrated several beneficial properties as an ideal drug-carrier, optimal drug-loading, and good long-term stability. NLCs are getting popular due to their stability advantages and the possibility to load various oil components either as an active or as a matrix. This review screens types of oils used till date in combination with solid lipids to form NLCs. These oils are broadly classified into two categories: Natural oils and Essential oils. NLCs offer range of advantages in drug delivery due to the formation of an imperfect matrix owing to the presence of oil. The type and percentage of oil used, determine optimal drug loading and stability. Literature shows that a variety of oils is/are used in NLCs mainly as the matrix, which is from natural origin, triglycerides class. On the other hand, essential oils not only serve as a matrix but also as an active moiety. In short, oil is the key ingredient in the formation of NLCs, hence it needs to be selected wisely as per the performance criteria expected. The aim of this article is to discuss shortly the role of liquid lipids and highlight the use of variety of oils in NLCs preparation.

Enhanced bactericidal effect of ceftriaxone drug encapsulated in nanostructured lipid carrier against gram-negative Escherichia coli bacteria: drug formulation, optimization, and cell culture study

BackgroundCeftriaxone is one of the most common types of antibiotics used to treat most deadly bacterial infections. One way to alleviate the side effects of medication is to reduce drug consumption by changing the ordinary drug forms into nanostructured forms. In this study, a nanostructured lipid carrier (NLC) containing hydrophilic ceftriaxone sodium drug is developed, and its effect on eliminating gram-negative bacteria Escherichia coli death is investigated.MethodsDouble emulsion solvent evaporation method is applied to prepare NLC. Mathematical modeling based on the solubility study is performed to select the best materials for NLC preparation. Haftyzer-Van Krevelen and Hoy’s models are employed for this purpose. Drug release from optimized NLC is examined under in vitro environment. Then, the efficacy of the optimized sample on eliminating gram-negative bacteria Escherichia coli is investigated.ResultsMathematical modeling reveals that both methods are capable of predicting drug encapsulation efficiency trends by chaining solid and liquid lipids. However, Haftyzer-Van Krevelen’s method can precisely predict the particle size trend by changing the surfactant types in water and oily phases of emulsions. The optimal sample has a mean particle size of 86 nm and drug entrapment efficiency of 83%. Also, a controlled drug release in prepared nanostructures over time is observed under in-vitro media. The results regarding the effectiveness of optimized NLC in killing Escherichia coli bacteria suggests that by cutting drug dosage of the nanostructured form in half, an effect comparable to that of free drug can be observed at longer times.ConclusionResults confirm that NLC structure is an appropriate alternative for the delivery of ceftriaxone drug with a controlled release behavior.

SCREENING STUDY FOR FORMULATION VARIABLES IN PREPARATION AND CHARACTERIZATION OF CANDESARTAN CILEXETIL LOADED NANOSTRUCTURED LIPID CARRIERS

The current study inspects the screening of the formulation components further, evaluates the physicochemical properties of the nanostructured lipid carriers (NLCs) for the antihypertensive drug as Candesartan Cilexetil (CC). The sequence screening of all excipients required for the preparation of NLCs should be performed. Firstly, the solubility of CC in different solid and liquid lipids is the major parameter for the selection of the best one. Precirol® ATO 5, Compritol ® 888 ATO and Glyceryl Monostearate (GMS) were showed the maximum solubility of the CC (1000±4.12 mg, 1500±4.15 mg and 1750±3.16 mg), respectively. Hence, they were selected as the solid lipids for the development of NLCs. Liquid lipids Transcutol® HP (30±2.21 mg/ml), Labrasol® ALF (25±1.32 mg/ml) and CapryolTM 90 (18±1.34 mg/ml) were observed to have good affinity for the drug on systematic screening of different liquid lipids. However, Precirol® ATO 5 was found to has good physical compatibility with Transcutol® HP, Compritol ATO 888 was found to has high physical miscibility with Labrasol® ALF and last GMS was appeared in good affinity and compatibly with CapryolTM 90. Hence, the following binary lipid mixtures (Precirol® ATO 5 - Labrasol® ALF), (Compritol® 888 ATO-Transcutol® HP) and (GMS - CapryolTM 90) were selected for the preparation of NLCs. The liquid–solid lipid mixture in the ratio up to 30:70 was observed to have sufficient melting point (55-59 0C). Lutrol F-68, Lutrol F-127, Cremophore EL and Cremophore® RH. In addition to, the combination of (Lutrol® F68:Cremophore® EL) and (Lutrol® F127: Cremophore® RH) were selected as the main surfactants for the preparation of NLCs formulations because of its good emulsification efficacy and homogeneity for the solid-liquid lipid mix. The prepared formulations were investigated for the different quality issues. All designed formulations observed in nanometer size of particles ranged from (408.9±11.5 to 114.6±8.3 nm) with high encapsulation efficiency around 99%. Also, the obtained results revealed that the ZP of the various formulations was consistently negative surface charge in between ((-13 ±2.3 to27.3±3.7 mV). Finally, formula number nine of CC (CC-NLC9) which composed of GMS (solid lipid), CapryolTM 90 (liquid lipid) and Lutrol® F127: Cremophore® RH (surfactants combination) was selected as the best formulation after the rank order for further investigations in the next work. &#x0D; Peer Review History: &#x0D; UJPR follows the most transparent and toughest ‘Advanced OPEN peer review’ system. The identity of the authors and, reviewers will be known to each other. This transparent process will help to eradicate any possible malicious/purposeful interference by any person (publishing staff, reviewer, editor, author, etc) during peer review. As a result of this unique system, all reviewers will get their due recognition and respect, once their names are published in the papers. We expect that, by publishing peer review reports with published papers, will be helpful to many authors for drafting their article according to the specifications. Auhors will remove any error of their article and they will improve their article(s) according to the previous reports displayed with published article(s). The main purpose of it is ‘to improve the quality of a candidate manuscript’. Our reviewers check the ‘strength and weakness of a manuscript honestly’. There will increase in the perfection, and transparency.&#x0D; Received file &#x0D; &#x0D; Average Peer review marks at initial stage: 5.0/10&#x0D; Average Peer review marks at publication stage: 7.5/10&#x0D; Reviewer(s) detail:&#x0D; Name: Dr. Mohammed Abdel-Wahab Sayed Abourehab&#x0D; Affiliation: Umm Al-Qura University; Makkah Al-Mukarramah, Saudi Arabia&#x0D; E-mail: maabourehab@uqu.edu.sa&#x0D; &#x0D; Name: Dr. Maha Khalifa Ahmed Khalifa &#x0D; Affiliation: Al-Azhar Universit - Cairo, Egypt&#x0D; E-mail: mahakhalifa.ahmed@hotmail.com&#x0D; &#x0D; Name: Dr. Evren Alğin Yapar&#x0D; Affiliation: Turkish Medicines and Medical Devices Agency, Turkiye&#x0D; E-mail: evren.yapar@yahoo.com&#x0D; Comments of reviewer(s): &#x0D; &#x0D; Similar Articles:&#x0D; FORMULATION AND CHARACTERIZATION OF TOPICAL NANO EMULGEL OF TERBINAFINE &#x0D; A REVIEW ON GOLD NANOPRTICLES SYNTHESIS AND CHARACTERIZATION &#x0D; FORMULATION AND EVALUATION OF ELASTIC LIPOSOMES OF DECITABINE PREPARED BY ROTARY EVAPORATION METHOD