Current Issue : April - June Volume : 2017 Issue Number : 2 Articles : 6 Articles
To overcome the disadvantage of the oral routes of antifungal fluconazole, new topical formulation was prepared in the form of solid lipid nanoparticles (SLNs) formulations. The fluconazole-SLNs were manufactured by modified high shear homogenization and ultrasonication method technique in which geleol was used as the solid lipid phase, tween 80, cremophor RH 40 and poloxamer 407 series as the surfactants. The produced fluconazole SLNs were characterized for particle size, zeta potential, entrapment efficiency, morphology by TEM and in-vitro release profiles. Also the optimized fluconazole-SLNs formulation was incorporated into carbopol gel and investigated for in-vitro antifungal activity. The results of the study revealed that fluconazole loaded SLNs showed extremely spherical shape having enriched core drug loading pattern with uniform particle size. A relatively high drug entrapment efficiency ranging from 41.45 to 77.94 % was obtained with zeta potential values lie between -24 to -29.8 mV indicating good stability. DSC examination revealed that fluconazole encapsulated in SLNs was in the amorphous state. In-vitro release study showed a sustained release of fluconazole from the SLNs up to 24 h following Higuchi order equations. In conclusion, SLNs with excellent particle size, high entrapment efficiency and controlled drug release can be produced representing a promising carrier for topical delivery of fluconazole....
Nystatin (NT) is an antibiotic which shows both fungistatic and fungicidal activity against a wide variety of yeasts and yeast-like fungi, including Candida albicans. Nystatins have very low permeation topically. NT also shows skin irritation by topical application. Thus the aim of present study was to increase solubility, permeability of NT and also reduce skin irritation by formulating a lyotropic liquid crystalline system. The liquid crystalline system of NT was formulated using glyceryl monooleate (GMO) / poloxamer 407 / water. The prepared liquid crystalline system was also compared with simple gel and emulgel of NT. The formulations were evaluated for phase identification, in-vitro and ex-vivo permeation study, texture characterization, skin irritation study, antifungal activity and stability studies. The optimized formulation F4 shows hexagonal phase identified by polarized light microscopy. In-vitro cumulative drug release of the optimized batch was 71.6 % and ex-vivo cumulative drug release was 50.01 % within 12 h. The antifungal inhibitory activity of optimized batch shows the highest zone of inhibition as compared to emulgel and simple carbopol gel. Skin irritation study suggested that prepared formulation shows no skin irritation upon topical administration. Furthermore the prepared optimized formulation was found to be stable....
The Mucoadhesive drug delivery system has occupied an important place in the field of\npharmaceutical research. Mucoadhesive tablets prolong the residence time of the drug at the site\nof application and provide extended therapeutic effect. Mucoadhesive tablets have been prepared\nfor various sites thus offering localization as swell as systemic control of drug release. The present\nstudy focuses on the concept of formulation of fluconazole as a mucoadhesive vaginal tablet, for\nimproving the sustained release of drug and localized action of the drug. Different polymers, such\nas Hydoxypropylmethylcellulose M 15, Carbopol71G-NFand Guar Gum were used with different\nconcentrations in order to get the desired sustained release profile over a period of more than12\nhrs. The tablets were prepared by direct compression method. All the formulations were evaluated\nfor crushing strength, friability, swelling behavior, adhesion time, drug content and in vitro drug\nrelease profile. All the formulation tested showed good physical and adhesive properties. It was\nfound that the controlled release rate of the formulation increases with increasing polymer\nconcentration. Kinetican modeling of release data supports an anomalous non-fickian release behavior. The antimycotic activity of selected formulations containing fluconazole (100 mg) was\ndetermined using an agar diffusion technique. Formulations tested showed activity against\nC. albicans....
Intestinal lymphatic drug delivery has been widely studied because drugs can bypass the first-pass metabolism in\nthe liver via the lymphatic route, which increases oral bioavailability. Various lipid-based nanoparticles have been\nused to deliver hydrophobic drugs to the lymphatic pathway. This review focuses on the liposomal delivery systems\nused for intestinal lymphatic drug transport. Liposomal formulations have attracted particular attention because\nthey can stimulate the production of chylomicrons and the incorporated drugs readily associate with enterocytederived\nchylomicrons, enhancing lymphatic drug transport. We believe that a full understanding of their contribution\nto intestinal drug translocation will lead to effective oral delivery with liposomal formulations....
The efficient delivery of therapeutic molecules to the cartilage of joints is a major obstacle in developing useful therapeutic interventions;\nhence, a targeted drug delivery system for this tissue is critical. We have overcome the challenge by developing a system that employs\nelectrostatic attraction between the negatively charged constituents of cartilage and a positively charged polymer, poly-beta amino esters\n(PBAEs). We have demonstrated cartilage uptake of dexamethasone (DEX) covalently bound to the PBAE was doubled and retention in\ntissues prolonged compared to the equivalent dose of the commercial drug formulation. Moreover, no adverse effects on chondrocytes were\nfound. Our data also show that PBAEs can bind not only healthy cartilage tissues but also enzymatically treated cartilage mimicking early\nstages of OA. Our PBAEs-prodrug technology's advantages are fourfold; the specificity and efficacy of its targeting mechanism for cartilage,\nthe ease of its production and the low-cost nature of the delivery system....
Glucan particles (GPs) are hollow, porous 3ââ?¬â??5 ...
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