Current Issue : October - December Volume : 2018 Issue Number : 4 Articles : 6 Articles
Paliperidone is a second generation antipsychotic agent, used in the treatment of schizophrenia. It is a hydrophobic drug which belongs to BCS class II and it has low bioavailability of about 28%. The present study was designed to improve the in-vitro dissolution properties of poorly soluble antipsychotic drug paliperidone by adopting the liquisolid technology. Liquisolids were prepared by powder solution technology using lactose as carrier, poly vinyl pyrolidone K25 as coating material, PEG 200, tween-80, propylene glycol as non-volatile solvents and sodium starch glycolate is used as a superdisintegrant. FTIR studies were carried out for all formulations. All prepared liquisolid compacts were subjected to weight variation, drug content uniformity, hardness, friability test, disintegration test and in-vitro dissolution tests. All the tested formulations showed higher drug dissolution than the pure drug. Optimized formulation LS8 containing tween-80 as solvent, lactose and PVP K25 in 10:1 ratio exhibited faster disintegration and desirable drug release of 99.15% in 45 min. Liquisolid technology is a promising method for solubility enhancement of paliperidone....
Raloxifene hydrochloride (RLH) was formulated into a pH-modified supersaturatable\nself-microemulsifying drug delivery system (S-SMEDDS) to increase drug solubility and dissolution\nrate. Optimal formulations of pH-modified S-SMEDDSs were developed by incorporating\nhydroxypropyl-cellulose-L as a precipitation inhibitor and phosphoric acid as a pH modifier (an\nacidifier). RLH was dissolved to greater extents by all pH-modified S-SMEDDSs compared with\nnon-pH-modified S-SMEDDSs. In particular, phosphoric acid afforded greater drug dissolution than\ndid the other acidifiers tested, perhaps because phosphoric acid better controlled the pH. More than\n50% of the RLH was released from the pH-modified S-SMEDDS at pH 2.5 compared with only ~5%\nof the drug into aqueous buffer (pH 1.2 or 6.8) after dissolution of a conventional tablet. pH-modified\nS-SMEDDSs with a hydrophilic polymer and phosphoric acid improved the dissolution behavior\nof a drug exhibiting poor aqueous solubility....
Poor solubility and bioavailability are limiting factors for the clinical application of curcumin. This study seeks to develop\npoloxamer/chitosan thermosensitive gel containing curcumin-cyclodextrin inclusion complex with enhanced brain bioavailability\nand antidepressant effect. The optimized gel had shorter gelation time and produced sustained release in vitro characterized\nwith non-Fickian diffusion. Pharmacokinetics of gel were evaluated using male Sprague-Dawley rats receiving 240...
Colloidal gold nanoparticles are targeting probes to improve varlitinib delivery into cancer\ncells. The nanoconjugates were designed by the bioconjugation of pegylated gold nanoparticles with\nvarlitinib via carbodiimide-mediated cross-linking and characterized by infrared and X-ray photoelectron\nspectroscopy. The drug release response shows an initial delay and a complete drug release after 72 h\nis detected. In vitro experiments with MIA PaCa-2 cells corroborate that PEGAuNPsVarl conjugates\nincrease the varlitinib toxic effect at very low concentrations (IC50 = 80 nM) if compared with varlitinib\nalone (IC50 = 259 nM). Our results acknowledge a decrease of drug side effects in normal cells and an\nenhancement of drug efficacy against to the pancreatic cancer cells reported....
Most free drugs that cross the bloodââ?¬â??brain barrier are characterized by high liposolubility, but they often have limited clinical\napplications because of poor dissolution and poor bioavailability. In this study, we prepared donepezil drug-loaded\nnanoparticles (DZP) with cholesterol-modified pullulan (CHP) as the nanocarrier (DZP-CHP) and surface modified the drugloaded\nnanoparticles to improve the water solubility of donepezil while enhancing its targeting and sustained release. We\ndetermined the drug loading and encapsulation efficiency of DZP-CHP nanoparticles at different feed ratios. The mean Ã?± SD\ndrug loading and entrapment efficiency were high: 13.52 Ã?± 2.03 and 86.54 Ã?± 1.31. On dynamic light-scattering measurement,\nmean Ã?± SD particle size was 260.7 Ã?± 1.76 nm, polydispersity index 0.123 Ã?± 0.004, and zeta potential âË?â??5.75 Ã?± 0.64 mV. DZP-CHP\nnanoparticles prepared with the optimal feed ratio (DZP : CHP= 1 : 5) were coated with polysorbate 80, and the adsorption\nprocess was determined by isothermal titration calorimetry. We found good affinity between polysorbate 80 and DZP-CHP,\nwith mean Ã?± SD coverage 2.7 Ã?± 0.372. The mean Ã?± SD drug loading and entrapment efficiency of polysorbate 80-emulsified\nDZP-CHP nanoparticles were 8.25 Ã?± 1.80 and 91.28 Ã?± 4.57, respectively, and the proportion of drug released by 72 h was 42.71%.\nCompared to DZP-CHP alone, PS-DZP-CHP can enhance the release of donepezil....
Felbinac, an active pharmaceutical ingredient (API) used clinically for the treatment\nof osteoarthritis, has poor solubility. Felbinac cataplasm product design was investigated using\nrheological and mechanical analyses. Experiments using a response surface methodology based\non Boxââ?¬â??Behnken design (BBD) incorporated three independent variables: the proportions of\npartially neutralized polyacrylate (NP800), dihydroxyaluminum aminoacetate (DAAA), and felbinac.\nStatistically significant quadratic models obtained using BBD demonstrated optimal NP-800,\nDAAA, and felbinac cataplasm proportions of 4.78ââ?¬â??5.75%, 0.30ââ?¬â??0.59%, and 0.70ââ?¬â??0.90%, respectively.\nFelbinac cataplasms exhibited ââ?¬Å?gel-likeââ?¬Â mechanical property with predominantly elastic behavior.\nRheological studies correlated increasing NP-800 and DAAA concentrations with increased complex\nmodulus (G*) values that were inversely related to peeling strength. Frequency sweep and creep tests\nrevealed decreasing tan Ã?¸ values with increasing NP-800 and DAAA concentrations. Gââ?¬â?¢ and Gââ?¬Â values\nwere higher for higher NP-800 and DAAA levels, although Gââ?¬Â values decreased with increasing\nDAAA concentration. Response surface methodology was applied to develop mathematical models.\nVariance analysis showed that the quadratic model effectively predicted felbinac and matrix material\ninteractions, with two verification samples upholding model predictions. Relative errors between\npredicted and measured G* values were 3.28% and 1.10% and for peeling strength were 1.24% and\n5.59%, respectively. In conclusion, rheological and mechanical analyses of felbinac cataplasms using\nBBD permits optimization of cataplasms as topical drug delivery vehicles....
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