Effect of Hydrophilic and Hydrophobic Polymers on Permeation of S-Amlodipine Besylate through Intercalated Polymeric Transdermal Matrix: 3(2) Designing, Optimization and Characterization.

OBJECTIVE: Innovations in material science, has made it possible to fabricate a pharmaceutical material of modifiable characteristics and utility, in delivering therapeutics at a sustained/controlled rate. The objective of this study is to design and optimize the controlled release transdermal films of S-Amlodipine besylate by intercalating hydrophilic and hydrophobic polymers.

METHODS: 3(2) factorial design and response surface methodology was utilized to prepare formulations by intercalating the varied concentration of polymers(A) and penetration enhancer(B) in solvent. The effect of these independent factors on drug release and flux was investigated to substantiate the ex-vivo, stability and histological findings of the study.

RESULTS: FTIR, DSC revealed the compatibility of drug with polymers, however, the semi-crystallinity in drug was observed under PXRD. SEM micrographs showed homogeneous dispersion and entanglement of drug throughout the matrix. Results from the permeation study suggested the significant effect of factors on the ex-vivo permeation of drug. It was observed that drug release was found to be increased with an increase in hydrophilic polymer concentration and PE. The formulations having polymers (EC:PVPK-30) at 7:3 showed maximum drug release with highest flux (102.60 ± 1.12µg/cm2/h) and permeability coefficient (32.78 ± 1.38cm/h). Significant effect of PE on lipid and protein framework of the skin was also observed which is responsible for increased permeation. The optimized formulation was found to be stable and showed no-sign of localized reactions, indicating safety and compatibility with the skin.

CONCLUSION: Thus, results indicated that the prepared intercalated transdermal matrix can be a promising non-oral carrier to deliver effective amounts of drug.