ABSTRACT
The aim of this study was to develop microemulgel for skin delivery of kojic acid. Microemulsions (ME) containing either oleic acid (OA) or caprylic/capric triglycerides as the basic oily components were developed after construction of pseudoternary phase diagrams. Tween 80 was used as surfactant for oleic acid system both in presence and absence of ethanol or propylene glycol (PG) as cosurfactants. For the caprylic/capric systems, Tween 85 was the surfactant in presence or absence of ethanol as cosurfactant. Selected ME formulations were tested for transdermal delivery of kojic acid both in fluid state and after transformation into gel. Incorporation of cosurfactants expanded the microemulsion zone. The cosurfactant free ME were more viscous. Incorporation of kojic acid in ME systems increased the transdermal flux compared to saturated aqueous solution. caprylic/capric ME were more efficient than (OA) based ME. Transformation of the tested ME systems into gel produced significant enhancement in transdermal drug delivery compared with the saturated aqueous drug solution. However, the data revealed superior efficacy for the fluid ME systems over the corresponding microemulgel. In conclusion, both (OA) and caprylic/capric ME were promising for dermal and transdermal delivery of kojic acid even after gel formation.
ABSTRACT
The objective of the current paper was to prepare and evaluate various polymeric films for fungal infection treatment and its impact on volunteer patients. Different Eudragit polymeric films containing Ketoconazole as antifungal drug were prepared by solvent casting technique. The prepared films were tested for their physicomechanical properties as tensile strength, physical endurance, elasticity, water vapor permeation and water loss. The release of ketoconazole from the prepared medicated films was examined. It is involved 20 volunteers suffering from legs fungal infection. Ten of the patients used the films and a follow up study was carried out for 14 days, in comparison with other patients who applied ketoconazole medicated ointment, cream gel and Emulgel. The results revealed that films prepared with Eudragit RL 100 containing glyceryl triacetate produced maximum release of ketoconazole both In vitro and In vivo as compared with other topical dosage forms as ointment, cream, gel and Emulgel. Moreover, the films constitute a simple and convenient method for treatment of various fungal infections. As conclusion, the use of antifungal drugs such as Ketoconazole incorporated in polymeric films, the output results provided promised evidence in the treatment of dermatophytosis.
ABSTRACT
Possible interaction between carbamazepine and different HPMC grades was done using DSC thermal analysis. The results indicated that the drug was compatible with these grades. Seven preparations of carbamazepine 200 mg controlled release tablets were prepared by wet granulation method and one preparation was prepared by direct compression method where different HPMC grades with different ratios were used. Concerning uniformity of weight, hardness and assay; all tablets conformed to pharmacopeal limits. Dissolution of the prepared tablets was done using basket method for 24 hours and paddle method for 4 hours. Tablets prepared by 30.0, 35.0 and 40.0% w/w HPMC K 100, 25.0% HPMC K 100 in combination with 5.0% HPMC K 4M and 15.0% w/w HPMC K 4M were conforming to USP limits, while tablets prepared by 15% K4M are not conforming to these limits. Tablets prepared by 12.5% HPMC K 15M by direct compression technique showed similar dissolution values to the innovator in five different media: distilled water, distilled water containing 1.0% SLS, buffer pH 1.2, acetate buffer pH 4.5 and phosphate buffer pH 6.8. The difference and similarity factors were found very acceptable. Scaling up of carbamazepine 200 mg controlled release tablets formulation from lab scale (500 tablets) to full production scale (500,000 tablets) was done. All the results of the scaling up were conforming to specifications and indicated that scaling up process has been done successfully and drug release kinetics indicated that the drug dissolution was zero order.