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Gupta M.,Drug Delivery Research Laboratory
Pharmaceutical development and technology | Year: 2013

Dermal delivery of fluconazole (FLZ) is still a major limitation due to problems relating to control drug release and achieving therapeutic efficacy. Recently, solid lipid nanoparticles (SLNs) were explored for their potential of topical delivery, possible skin compartments targeting and controlled release in the skin strata. The retention and accumulation of drug in skin is affected by composition of SLNs. Hence, the aim of this study was to develop FLZ nanoparticles consisted of various lipid cores in order to optimize the drug retention in skin. SLNs were prepared by solvent diffusion method and characterized for various in vitro and in vivo parameters. The results indicate that the SLNs composed of compritol 888 ATO (CA) have highest drug encapsulation efficiency (75.7 ± 4.94%) with lower particle size (178.9 ± 3.8 nm). The in vitro release and skin permeation data suggest that drug release followed sustained fashion over 24 h. The antifungal activity shows that SLNs made up of CA lipid could noticeably improve the dermal localization. In conclusion, CA lipid based SLNs are represents a promising carrier means for the topical treatment of skin fungal infection as an alternative to the systemic delivery of FLZ. Source


Tiwari S.,Drug Delivery Research Laboratory | Agrawal G.P.,Drug Delivery Research Laboratory | Vyas S.P.,Drug Delivery Research Laboratory
Nanomedicine | Year: 2010

The mucosal immune system, the primary portal for entry of most prevalent and devastating pathogens, is guarded by the special lymphoid tissues (mucosally associated lymphoid tissues) for immunity. Mucosal immune infection results in induction of IgA-manifested humoral immunity. Cell-mediated immunity may also be generated, marked by the presence of CD4+ Th1 and CD8+ cells. Furthermore, the immunity generated at the mucosal site is transported to the distal mucosal site as well as to systemic tissues. An understanding of the molecular basis of the mucosal immune system provides a unique platform for designing a mucosal vaccine. Coadministration of immunostimulatory molecules further accelerates functioning of the immune system. Mimicking receptor-mediated binding of the pathogen may be achieved by direct conjugation of antigen with an immunostimulatory molecule or encapsulation in a carrier followed by anchoring of a ligand having affinity to the cells of the mucosal immune system. Nanotechnology has played a significant role in mucosal vaccine development and among the available options liposomes are the most promising. Liposomes are phospholipid bilayered vesicles that can encapsulate protein as well as DNA-based vaccines and offer coencapsulation of adjuvant along with the antigen. At the same, time ligand-conjugated liposomes augment interaction of antigen with the cells of the mucosal immune system and thereby serve as suitable candidates for the mucosal delivery of vaccines. This article exhaustively explores strategies involved in the generation of mucosal immunity and also provides an insight to the progress that has been made in the development of liposome-based mucosal vaccine. © 2010 Future Medicine Ltd. Source


Paliwal S.R.,Drug Delivery Research Laboratory | Paliwal R.,Drug Delivery Research Laboratory | Agrawal G.P.,Pharmaceutics Research Laboratory | Vyas S.P.,Drug Delivery Research Laboratory
Nanomedicine | Year: 2011

Liposomes are well-established nanocarriers for improving the therapeutic index of anticancer agents. A remarkable understanding in the pathophysiology of breast cancer progression has emerged with information on the involved specific biomolecules, which may serve as molecular targets for its therapy. Hormonal and nonhormonal receptors can both be exploited for targeting to breast cancer cells. Targeted delivery of cytotoxic drugs using liposomes is a novel approach for breast cancer therapy. In the present article, we summarize molecular targets present on the breast cancer cells. Recent developments in liposome-based delivery of bioactives for selective treatments of breast cancer are discussed. In addition, utilization of bioenvironmental conditions of tumor for liposome-based targeted delivery is also summed up. © 2011 Future Medicine Ltd. Source


Gupta M.,Drug Delivery Research Laboratory | Vyas S.P.,Drug Delivery Research Laboratory
Chemistry and Physics of Lipids | Year: 2012

The nanoparticulate carrier systems as solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) have gained interest for the topical treatment of skin associated fungal infection as they facilitate the skin penetration of loaded drugs. Therefore in this study, SLNs and NLCs loaded fluconazole (FLZ) were prepared by solvent diffusion method in an aqueous system and characterized for different parameters. In addition, antifungal activity was carried out on experimentally induced cutaneous candidiasis in immunosuppressed albino rats. The results showed that SLNs and NLCs represent the respective mean particle sizes of approx. 178 and 134 nm with encapsulation efficiency of 75.7 ± 4.94% and 81.4 ± 3.89%, respectively. The skin-retention studies of FLZ from in vitro and in vivo experiments revealed significantly higher accumulation of drug in the case of NLCs formulation. The in vivo cumulative amount of FLZ retention from NLCs was more than 5-fold that of the plain solution, while it was 3.3-fold more in the case of an equivalent-dose application in the form of SLNs at 12 h after administration. The antifungal study also confirmed the maximum therapeutic efficacy of NLCs, as the lowest number of cfu/ml was recorded. It can be concluded from this study that NLCs provide a good skin targeting effect and may be a promising carrier for topical delivery of FLZ offering the sustained release and maintain the localized effect, resulting in an effective treatment of a life-threatening cutaneous fungal infection. © 2012 Elsevier Ireland Ltd. Source


Gupta M.,Drug Delivery Research Laboratory | Agrawal G.P.,Drug Delivery Research Laboratory | Vyas S.P.,Drug Delivery Research Laboratory
Current Molecular Medicine | Year: 2013

Inspite of demanding research that has been undertaken for cancer treatment, cancer is a major cause of mortality. Available conventional treatment options of solid tumor are associated with serious side effects. Nanomedicines mediated fascinating approach may be effectively utilized for efficient tumor targeting by avoiding all the problems associated with conventional chemotherapy. Polymeric nanomedicines such as polymer micelles, polymeric nanoparticles, polymersomes and polymer conjugates currently developed for solid tumor treatment have proved to be efficacious cancer therapeutics. These polymeric nanostructures are able to reach tumor tissue or angiogenic endothelial cells either passively or actively. To date, more advancement in the tumor targeting field includes stimuli sensitive polymeric nanocarriers that pass through the intracellular delivery barriers and release the bioactives in response to the microenvironmental trigger of tumor cell. This review discusses the molecular aspects of solid tumor pathophysiology and its dramatic impact on research for innovative and novel therapeutic approaches linked with tumor-targeting polymeric nanomedicines. © 2013 Bentham Science Publishers. Source

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