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The management of the central nervous system (CNS) disorders is challenging, due to the need of drugs to cross the blood‒brain barrier (BBB) and reach the brain. Among the various strategies that have been studied to circumvent this challenge, the use of the intranasal route to transport drugs from the nose directly to the brain has been showing promising results. In addition, the encapsulation of the drugs in lipid-based nanocarriers, such as solid lipid nanoparticles (SLNs), nanostructured lipid carriers (NLCs) or nanoemulsions (NEs), can improve nose-to-brain transport by increasing the bioavailability and site-specific delivery. This review provides the state-of-the-art of
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To reduce the problems of poor solubility, high in vivo dosage requirement, and weak targeting ability of paclitaxel (PTX), a hyaluronic acid-octadecylamine (HA-ODA)-modified nano-structured lipid carrier (HA-NLC) was constructed. HA-ODA conjugates were synthesized by an amide reaction between HA and ODA. The hydrophobic chain of HA-ODA can be embedded in the lipid core of the NLC to obtain HA-NLC. The HA-NLC displayed strong internalization in cluster determinant 44 (CD44) highly expressed MCF-7 cells, and endocytosis mediated by the CD44 receptor was involved. The HA-NLC had an encapsulation efficiency of PTX of 72.0%. The cytotoxicity of the PTX-loaded nanoparticle HA-NLC/PTX in MCF-7 cells was much stronger than that of the commercial preparation Taxol®. In vivo, the HA-NLC exhibited strong tumor targeting ability. The distribution of the NLCs to the liver and spleen was reduced after HA modification, while more nanoparticles were aggregated to the tumor site. Our results suggest that HA-NLC has excellent properties as a nano drug carrier and potential for in vivo targeting.
ABSTRACT
To reduce the problems of poor solubility, high in vivo dosage requirement, and weak targeting ability of paclitaxel (PTX), a hyaluronic acid-octadecylamine (HA-ODA)-modified nano-structured lipid carrier (HA-NLC) was constructed. HA-ODA conjugates were synthesized by an amide reaction between HA and ODA. The hydrophobic chain of HA-ODA can be embedded in the lipid core of the NLC to obtain HA-NLC. The HA-NLC displayed strong internalization in cluster determinant 44 (CD44) highly expressed MCF-7 cells, and endocytosis mediated by the CD44 receptor was involved. The HA-NLC had an encapsulation efficiency of PTX of 72.0%. The cytotoxicity of the PTX-loaded nanoparticle HA-NLC/PTX in MCF-7 cells was much stronger than that of the commercial preparation Taxol®. In vivo, the HA-NLC exhibited strong tumor targeting ability. The distribution of the NLCs to the liver and spleen was reduced after HA modification, while more nanoparticles were aggregated to the tumor site. Our results suggest that HA-NLC has excellent properties as a nano drug carrier and potential for in vivo targeting.
ABSTRACT
@#Introduction: Hepatocellular carcinoma is one of the most common cancers that affected human in more than half of the world population. Although there is yet any alternatives treatment found for this disease, the antitumor property of thymoquinone has been well studied in most of cancer cell lines. Nonetheless, poor bioavailability of TQ limits its efficiency. The encapsulation form of TQ, TQ-NLC is suggested to enhance its bioavailability as well as cytotoxicity towards cancer cells via increasing resistance time and targeting drug to specified location in the body. Therefore, it is a great advantage to look at the effects of TQ-NLC towards HepG2. This study is design to look at the anti-proliferative effect of TQ-NLC on HepG2 and the changes in the cells morphology. Methods: Both cells were bought from ATCC and cultured in supplemented DMEM. Cell viability was determined via MTT assay. Pro-apoptotic effect of TQ-NLC was further confirmed with Annexin V staining. Morphology hallmarks of apoptosis of treated cells were also analysed using inverted microscope. Images were captured at 24, 48 and 72 hours. Results: TQ-NLC was very potent towards HepG2 compared to 3T3 with the relative IC50 of 25 µM. TQ-NLC was also more potent compared to the non-encapsulated form, TQ. Further analysis confirmed that TQ-NLC capable to increase the percentage of apoptotic cells in time-dependent manner. Qualitatively, all treated cells displayed the apoptosis morphology with increasing concentration and longer time-point. Conclusion: TQ-NLC showed greater cytotoxic effects towards HepG2 which was further confirmed with the morphological analysis
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NeoplasmsABSTRACT
The HIV/AIDS pandemic is an increasing global burden with devastating health-related and socioeconomic effects. The widespread use of antiretroviral therapy has dramatically improved life quality and expectancy of infected individuals. But currently available drug regimens and dosage forms are not good enough to eradicate HIV. Suboptimal adherence, toxicity, drug resistance and viral reservoirs make the lifelong treatment of HIV infection challenging. Along with some other organs, highly vascularized and secured with blood-brain barrier (BBB), brain acts as a great reservoir for the HIV virus. But all the available drug delivery techniques are not capable of bypassing the BBB and deliver anti-HIV drugs to the brain. In this review, all the brain delivery techniques available till date has been reviewed and recent noble ideas for delivering anti-HIV drugs to brain has been discussed.
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The aim of this study was to prepare and evaluate gels incorporating nanostructured lipid carriers (NLC) of Miconazole nitrate (MN) for systemic delivery of the active after topical application. MN has been used as model drugs to be incorporated into nanostructured lipid carriers, once they are very well established as antimycotics for the treatment of topical fungal infections. NLC designed for topical administration of MN, were prepared by the hot high pressure homogenization technique. This MN-NLC was characterized for particle size, entrapment efficiency, and SEM. The lipid nanoparticles were incorporated in gels for convenient topical application and were evaluated forfor particle size, Rheological analysis Texture analysis , In vitro drug release studies and Ex Vitro skin permeation Studies. The preparation of aqueous NLC dispersions with a mean particle size lower than 300 nm has been obtained with uniform size distribution (PI < 0.350). The prepared semi-solid systems showed mean particle size remained lower than 250 nm and PI remained lower than 0.500 after 3 months of storage. An initial rapid release was observed in the case of Marketed gel, whereas MN- NLC Gel depicted a slow initial release with a lag time of 0.5 h and 1 h, respectively. High amount of MN release was facilitated through abdominal skin of rats from marketed gel than MN-NLC Gel. Research work could be concluded as successful development of MN-loaded NLC-bearing hydrogel to increase the encapsulation efficiency of colloidal lipid carriers with advantage of improved performance in terms of stability and provides a sustaining MN topical effect as well as faster relief from fungal infection.