Solid Lipid Carriers Research Articles

Lipid-based nanodelivery systems of curcumin: Recent advances, approaches, and applications

Despite its many beneficial effects, pharmaceutical applications of curcumin (CUR) are limited due to its chemical instability, low solubility/absorption and weak bioavailability. Recent advances in nanotechnology have enabled the development of CUR-loaded nanodelivery systems to tackle those issues. Within many different nanocarriers developed for CUR up to date, lipid-based nanocarriers (LBNs) are among the most extensively studied systems. LBNs such as nanoemulsions, solid lipid carriers, nanostructured phospholipid/surfactant carriers are shown to be potential delivery systems capable of improving the solubility, bioavailability, and chemical stability of CUR. The particle characteristics, stability, bioavailability, and release properties of CUR-loaded LBNs can be tailored via optimizing the formulation and processing parameters. This paper reviews the most recent studies on the development of various CUR-loaded LBNs. Approaches to the improvement of CUR bioavailability and release characteristics of LBNs are discussed. Furthermore, challenges in the development of CUR-loaded LBNs and their potential applications are presented.

Novel Herbal Nanocarriers for Treatment of Dermatological Disorders.

In the present scenario, the use of novel nanocarriers to provide a better therapy regimen is noteworthy. Nanotechnology with the advanced system enables the herbs for encapsulation within the smart carrier and boosts the nanotherapeutic. These emerging innovations of herbal nanocarriers have paved the way for dermal targeting by eliciting the desired response for particular diseases. In this current manuscript, an extensive search is conducted for the original research papers using databases, viz., Google Scholar, PubMed, Science Direct, etc. Furthermore, painstaking efforts are made to compile and update the novel herbal nanocarriers, such as liposomes, ethosomes, transferosomes, niosomes, nanoemulsions, nanogels, nanostructured lipid carriers, solid lipid carriers, etc., which are mostly used for the treatment of several skin maladies, viz., eczema, psoriasis, acne, etc. This article highlights the recent findings that the innovators are exclusively working on herbal drug delivery systems for dermal targeting, and these are enumerated in the form of tables. Herbal formulations employing a suitable nanocarrier could be a promising approach for the treatment of several pathological conditions, including skin ailments. Therefore, scientific research is still being carried out in this specific area for a better perspective in herbal drug delivery and targeting.

Nanocarriers(s) Based Approaches in Cancer Therapeutics

Nanomedicine is an emerging field, which constitutes a new direction in the treatment of cancer. The advent of nanotechnology has the potential to greatly facilitate the early detection and treatment of cancer. Nanocarriers are a group of nano-sized vehicles devised to deliver loaded bioactive(s) to target malignant cells, tissues or organs and have provided remarkably improved therapeutic efficacy for cancer therapy. A variety of nanocarriers(s)such as dendrimers, nanoparticle(s), liposomes, micelles, gold carriers, solid lipid carriers, carbon nanotubes, magnetic carriers and viral carriers, incorporating cytotoxic therapeutics have emerged as striking delivery system(s) in the area of cancer research. To improve the biological distribution of therapeutic bioactive(s), some modified carriers have designed to accommodate efficient loading and release of drugs with a wide spectrum of chemical and physical characteristics. In addition, physicochemical modifications of the surface or interior of NPs allow for modulation of pharmacokinetic features as per clinical demands. However, cancer-related mortality still remains high and drug-mediated cancer treatment is a challenging research field despite the remarkable advances in targeting efficiency and therapeutic efficacy demonstrated and resulted from NPs.This review focuses primarily on current nano drug delivery systems for cancer therapy. The current challenges related to therapeutic nanomedicines, as well as critical analysis of the different delivery nanoparticles, are also discussed.

Advancements in nanotherapeutics for Alzheimer's disease: current perspectives.

ObjectivesConsiderable progress has been made in the treatment of Alzheimer's disease (AD), but all available strategies focus on alleviating symptoms rather than curing, which means that AD is viewed as an unresolvable neurodegenerative disease. Nanotechnological applications offer an alternative platform for the treatment of neurodegenerative diseases. This review aims to summarize the recent nanomedicine and nanotechnology developments for the treatment of AD. Key findingsA plethora of nanocarriers and nanoparticle prodrugs have been reported to have negligible cytotoxicity in animal models, and these developments have revealed new opportunities for development of new classes of potent drug formulations for AD. Different nanotechnology-based approaches such as polymers, emulsions, lipo-carriers, solid lipid carriers, carbon nanotubes and metal-based carriers have been developed over the past decade, and they have been focusing on both neuroprotective and neurogenerative techniques to treat AD. Studies also reveal that nanotechnological approaches can aid in early diagnosis of AD and enhance therapeutic efficacy and bioavailability. SummaryNotably, the drugs used conventionally to target the central nervous system have limitations that include an inability to cross the 'blood-brain barrier' or the 'blood-cerebrospinal fluid barrier' effectively and high drug efflux due to the activity of P-glycoprotein, but these limitations can be successfully overcome when nanocarriers are used for targeted drug delivery in AD.

Development and Optimisation of Spironolactone Nanoparticles for Enhanced Dissolution Rates and Stability

Stable solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) formulations to enhance the dissolution rates of poorly soluble drug spironolactone (SP) were being developed. Probe ultra-sonication method was used to prepare SLNs and NLCs. All NLCs contained stearic acid (solid lipid carrier) and oleic acid (liquid lipid content), whereas, SLNs were prepared and optimised by using the solid lipid only. The particles were characterised in terms of particle size analysis, thermal behaviour, morphology, stability and in vitro release. The zeta sizer data revealed that the increase in the concentration of oleic acid in the formulations reduced the mean particle size and the zeta potential. The increase in concentration of oleic acid from 0 to 30% (w/w) resulted in a higher entrapment efficiency. All nanoparticles were almost spherically shaped with an average particle size of about ∼170 nm. The DSC traces revealed that the presence of oleic acid in the NLC formulations resulted in a shift in the melting endotherms to a higher temperature. This could be attributed to a good long-term stability of the nanoparticles. The stability results showed that the particle size remained smaller in NLC compared to that of SLN formulations after 6 months at various temperatures. The dissolution study showed about a 5.1- to 7.2-fold increase in the release of the drug in 2 h compared to the raw drug. Comparing all nanoparticle formulations indicated that the NLC composition with a ratio of 70:30 (solid:liquid lipid) is the most suitable formulation with desired drug dissolution rates, entrapment efficiency and physical stability.

Nanocarriers Usage for Drug Delivery in Cancer Therapy.

Conventional therapeutic agents have displayed significant shortcomings. For this reason, important achievements have effectively made in biotechnology for delivering the therapeutic agents to the site of action, and diminish side effects. Polymeric carriers, micelles, dendrimers, liposomes, solid lipid carriers, gold carriers, viral carriers, nanotubes and magnetic carriers incorporating cytotoxic therapeutics have developed. To improve biological distribution of therapeutic drugs, some modified carriers have designed in optimal size and modified surface area. Delivery of carriers to target cells could be done by passive and active targeting.

Characterization of Celecoxib-Loaded Solid Lipid Nanoparticles Formulated with Tristearin and Softisan 100

Purpose: To prepare solid lipid nanoparticles employing softisan 100 (SOFTI) or tristearin (TS) as solid lipid carriers for celecoxib (CXB) to overcome its dissolution challenge.Methods: The solid lipid nanoparticles (SLN) of CXB were prepared by ultrasonic melt-emulsification technique. SLN was characterized using differential scanning calorimetry (DSC), Fourier transform infra spectroscopy (FTIR), as well as for entrapment efficiency, particle size, zeta potential and CXB release.Results: The SLN formulations exhibited high CXB entrapment efficiency (91.6 % for SOFTI and 94.6 % for TS) while mean particle size was 181.0 ± 4.6 and 346.3 ± 3.8 nm for SOFTI and TS, respectively. The DSC thermograms showed the disappearance of CXB peak due to its molecular distribution in the lipid nanoparticles while FTIR spectra revealed physical interaction of CXB with the tested lipids. The tendency of SOFTI to liberate CXB in 24 h was higher than that of TS (55.5 ± 1.07 vs 49.2 ± 2.94 %, p < 0.05). Drug release was by non-Fickian mechanism.Conclusion: Formulation of CXB in SLN using TS or SOFTI produces sustained drug release delivery that can overcome the dissolution limitation of the drug and thus, improve its therapeutic efficacy.Keywords: Celecoxib, Solid lipid nanoparticles, Tristearin, Softisan, Dissolution limitation, Sustained drug release

Tailoring nanostructured solid-lipid carriers for time-controlled intracellular siRNA kinetics to sustain RNAi-mediated chemosensitization

Use of siRNA for silencing major oncogenic/chemoresistance targets such as survivin has strong potential for cancer therapy. However, a key clinical limitation is their short action, preventing them from sustaining their therapeutic RNA-interference activity for optimal chemosensitization. This issue is tackled from the perspective of intracellular siRNA kinetics using a novel lipid-based “nanostructured siRNA carrier” (NSC), which incorporates variable amount of oil phase into the solid-lipid matrix to modify its siRNA release behaviors. We demonstrate that by manipulating the degradation responses of NSC device to lysosomal enzyme, tailoring of intracellular siRNA kinetics is achievable. A tailored NSC design delivering survivin-siRNA can extend the survivin knockdown period to 9 days, translating into steady, effective in vitro and in vivo chemosensitization of prostate cancer to docetaxel for over a week. All in all, this new NSC design provides a convenient mean to set up a clinically more appealing weekly or longer dosing cycle for siRNA therapy, which addresses a significant unmet need for prostate cancer treatment and is potentially useful for other chronic disease conditions as well.

Current View on Nanosized Solid Lipid Carriers for Drug Delivery to the Skin

Drug delivery into the skin is problematic because, as a natural barrier, it has a very low permeation rate. Several approaches have been made to increase the latter. Current advances in materials science and nanotechnology promise the development of new generations of drug carriers for therapeutic, diagnostic and protective purposes. We have reviewed various lipid drug delivery systems to the skin, with the main focus on solid lipid nanoparticles (SLNs). Further the article concerns possible variants in formulation of SLNs, the selection of lipid compounds and safe stabilizers, and the influence of the physicochemical properties of the drugs on distribution after loading into SLNs. In the last part the advantages of delivery into keratinocytes by SLNs over that of the free drug is addressed, focusing on decreased cytotoxicity of the incorporated drug in SLNs and controlled drug delivery to the subcellular compartments. This knowledge is important in the design and production of advanced solid lipid drug carriers. Additionally, the need for novel approaches or devices to improving permeation is also discussed in the context of moving the nanocarriers to targets deeper in the skin.

Solid Lipid Nanoparticles and Nanostructured Lipid Carriers – Innovative Generations of Solid Lipid Carriers

The first generation of solid lipid carrier systems in nanometer range, Solid Lipid Nanoparticles (SLN), was introduced as an alternative to liposomes. SLN are aqueous colloidal dispersions, the matrix of which comprises of solid biodegradable lipids. SLN are manufactured by techniques like high pressure homogenization, solvent diffusion method etc. They exhibit major advantages such as modulated release, improved bioavailability, protection of chemically labile molecules like retinol, peptides from degradation, cost effective excipients, improved drug incorporation and wide application spectrum. However there are certain limitations associated with SLN, like limited drug loading capacity and drug expulsion during storage, which can be minimized by the next generation of solid lipids, Nanostructured lipid carriers (NLC). NLC are lipid particles with a controlled nanostructure that improves drug loading and firmly incorporates the drug during storage. Owing to their properties and advantages, SLN and NLC may find extensive application in topical drug delivery, oral and parenteral administration of cosmetic and pharmaceutical actives. Cosmeceuticals is emerging as the biggest application target of these carriers. Carrier systems like SLN and NLC were developed with a perspective to meet industrial needs like scale up, qualification and validation, simple technology, low cost etc. This paper reviews present status of SLN and NLC as carrier systems with special emphasis on their application in Cosmeceuticals; it also gives an overview about various manufacturing techniques of SLN and NLC.

Solubility of carbon dioxide in three lipid-based biocarriers

Equilibrium data of the solubility of carbon dioxide in Precirol ® ATO5, Compritol ® 888 ATO and Gelucire ® 43-01, three solid lipid carriers suitable for controlled/sustained delivery, were measured by a static analytical method for three different temperatures each, in a pressure range from 10 to 20 MPa. The influence of the presence of carbon dioxide in the melting point of the lipid matrices was also studied by a visual method for pressures up to 30 MPa. All the compounds studied presented a similar behaviour in the presence of carbon dioxide, showing a decrease in the melting points between 5 and 13 °C, whereas the solubility of carbon dioxide varies from 0.3 to 0.5 g/g of lipid compound. These results are of utmost importance to design supercritical fluid processes for particle formation at lower operating costs.

Formulation and in vitro-in vivo evaluation of piribedil solid lipid micro- and nanoparticles

Modification of the dissolution rate and, thus, the enhancement of the bioavailability of a dopaminergic drug, piribedil, which has a low aqueous solubility and short elimination half-life have been the aim in this study. Preparations of micron and submicron particles using solid lipid carriers have been performed for this purpose. For the avoidance of solvent residues resulting from the preparation technique, cold and hot homogenization methods have been used to prepare solid lipid particles. After obtaining an appropriate particle size, piribedil loading and preparation yield by the use of those two methods, various formulations have been prepared with different lipid, drug and surfactant materials. The factors mentioned were found to affect properties of the particles, and the release rate was found to be the fastest in acidic medium. Suspensions of pure piribedil and a formulation, selected according to the results obtained from in vitro dissolution and particle size experiments, were compared using tremor tests in mice. The same suspensions were applied perorally to rabbits and bioavailability of the solid lipid particle was found to be higher than the pure piribedil. After an in vitro-in vivo evaluation of piribedil solid lipid particles developed for Parkinson's disease therapy, it has been determined that release rate could be controlled and piribedil bioavailability could be improved.