Current Issue : January - March Volume : 2018 Issue Number : 1 Articles : 5 Articles
The aim of the study was to develop a reservoir-type transdermal patch for a controlled delivery of dexibuprofen and to evaluate\nits in vivo anti-inflammatory activity in Albino Wistar rats. In order to develop these patches, six formulations of dexibuprofen\nmicroemulsion comprising ethyl oleate, Tween 80: PG (2 : 1), and water were prepared by simplex lattice design and characterized.\nThe reservoir compartment was filled with these microemulsions and in vitro release and skin permeation were assessed. The\noptimized patch was obtained on the basis of the responses: ...
The aim of the present study was to develop and optimize the self-microemulsifying drug delivery formulation of\nbosentan monohydrate (BM) and assess the pharmacokinetic parameters in rats. Poor aqueous solubility of bosentan\nmonohydrate (BM) is a major determinant of its low oral bioavailability. Screening of various components of SMEDDS was done\nby solubility study. Clove oil as oil, tween 80 and labrasol as surfactants, PEG 400 as co-surfactant and ethanol (99.5 %w/v) as\nco-solvent to minimize the chance of drug precipitation were chosen for SMEDDS formulation. Pseudoternary phase diagram\nwas plotted to identify the self-emulsification region and surfactant to co-surfactant ratio. Further formulation was optimized by\napplying D-optimal mixture design with three independent variables X1 (Oil %w/w), X2 (Surfactants %w/w) and X3 (cosurfactant\n%w/w). Predicted compositions were evaluated for two responses: globule size (nm) and %transmittance.\nEnhancement of bioavailability was confirmed by pharmacokinetic study in rats. Optimized batch containing 12.5 mg of BM drug\nloading was predicted to 9% w/w clove oil, 56% w/w surfactant mixture (tween 80 and labrasol), 33% w/w PEG 400 and\n2%w/w ethanol (99.5%w/w) using design. Responses were predicted to 15.29 nm globule size and 99.7 % transmittance with\n0.976 batch desirability. Good agreement was observed between experimental and predicted responses. From the\nbioavailability study it was found that BM SMEDDS shows 2.55 times improvement in oral bioavailability compared to standard\nsuspension of BM in rats....
The aim of this study was to prepare and characterize an innovative hepatocellular carcinoma-targeted therapeutic drug\ndelivery system based on folate-PEG-mesoporous silica nanoparticles (FA-PEG-MSNs) loaded with paclitaxel (PTX). In vitro cell\nexperiments and an in vivo antitumor efficacy study demonstrated that FA-PEG-MSNs-PTX produced significantly higher tumor\ninhibition compared with pure PTX and mesoporous silica nanoparticles loaded with paclitaxel (MSNs-PTX). The biodistribution\ninvestigation of PTX in nude mice revealed that the FA-PEG-MSNs-PTX could accumulate in tumors. Folic acid functionalized\nMSNs resulted in a good targeting effect, confirming that FA-PEG-MSNs-PTX is a promising tumor-targeted drug delivery system\nfor liver cancer chemotherapy....
Cell type, morphology, and functioning are key variables in the construction of efficient ââ?¬Å?drug-vehicleââ?¬Â hybrids in magnetic drug\ndelivery. Iron-encapsulated multiwall carbon nanotubes (Fe@MWCNTs) appear as promising candidates for theranostics due to\nin situ chemical catalytic vapor deposition (c-CVD) synthesis, straightforward organic functionalization, and nanoneedle (1D)\nbehavior. Here, model hybrids were synthesized by exploring C-sp2 chemistry ((1+2)-cycloaddition of nitrenes and amidation) of\nthe outer MWCNT walls combined with anticancer agents, that is, 5-fluorouracil (5FU), purpurin (Purp), and 1,8-naphthalimide\nDNA intercalators (NIDIs), via linkers. Analyses of the Fe@MWCNT vehicles by SEM, TEM, and Raman spectroscopy revealed\ntheir morphology whileMÃ?¨ossbauer spectroscopy confirmed the presence of encapsulated ferromagnetic iron-based nanodomains.\nCytotoxicity of the hybrids was studied using a 24 h MTS assay combined with the apoptosis and life cycle assays against human\nmelanoma (Me45), colon carcinoma (HCT116+), and colon adenocarcinoma (Caco-2). The cells had different sensitivity to the\nvehicles themselves as well as to the hybrids. MWCNT-based covalent hybrids of 5FU and Purp emerged as the most promising\nsystems against Me45 and HCT116+ cell lines with the highest in vitro cytotoxicity and proapoptotic activity. Furthermore,\nnanotubes bearing 4-nitro- and 4-(N-morpholinyl)-1,8-naphthalimide DNA intercalators appear as a promising candidate for the\ntreatment of Caco-2....
Thermosensitive hydrogels have increasingly received considerable attention for local drug delivery based on many advantages.\nHowever, burst release of drugs is becoming a critical challenge when the hydrogels are employed. Microspheres- (MS-) loaded\nthermosensitive hydrogels were thus fabricated to address this limitation. Employing an orthogonal design, the spray-dried\noperations of tenofovir (TFV)/Bletilla striata polysaccharide (BSP)/chitosan (CTS) MS were optimized according to the drug\nloading (DL).Thephysicochemical properties of the optimalMS(MS F)were characterized.Depending on the gelation temperature\nand gelating time, the optimal CTS-sodium alginate- (SA-) ...
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