Formulation and Evaluation by Appling 32 (Three Squire) Factorial Design of Lercanidipine Hydrochloride Buccal Tablets with Mucoadhesive Polymers

Abstract:

Aim: The aim of the present research work is to develop buccal tablets of Lercanidipine hydrochloride to reduce dosage frequency; obtain optimized and controlled therapy, better patient compliance. Materials and Methods: Lercanidipine HCL was obtained as a gift sample from Sun Pharma, Baroda, India. Other ingredients like Na-alginate, Carbopol 934 P, Micro Crystalline Cellulose, Mannitol, Magnesium stearate, Ethyl cellulose and Hydroxy Propyl Methyl CelluloseK4M were purchased from various sources. All other ingredients used were of analytical grade. Attempt was made by using mucoadhesive polymers HPMC K4 M, sodium alginate and carbopol 934 P in combination with Ethyl Cellulose as an impermeable backing layer. Results: Combination of polymer HPMC K4 M and sodium alginate release of drug was found in desired manner than other combinations. On the basis of the preliminary trials a 3² full factorial design was employed to study the effect of independent variables such as concentration of sodium alginate: HPMC K4M (X1) and type of filler (X2) on dependent variables. Factorial batches of F1 to F9 were formulated. HPMC K4M exhibited a much greater sustained effect on the release rate compared with sodium alginate. F4 shown the highest f2 value 70.46 and also all the h drug release was within the specified range. Based on the f2 value and targeted release profile the F4 batch was considered as optimized batch. Formulation F4 was subjected to an in vitro buccal permeation study. The results showed drug permeation of 99.04% in 12 h. The correlation between in vitro drug release rate and in vitro drug permeation across the chicken mucosa was found to be positive, with a correlation coefficient (R2) of 0.9921. Conclusion: From kinetic modelling of the dissolution profile of the optimized formulation, it was concluded that there is erosion-controlled release of Lercanidipine from the buccal adhesive drug delivery system.

Key words: Lercanidipine hydrochloride, Buccal tablets, HPMC K4M, Buccal permeation study, Erosion controlled release.