Rahul Maheshwari, Piyoosh Sharma, Muktika Tekade, Umesh Atneriya, Kamal Dua, Philp M. Hansbro and Rakesh K. Tekade* Pages 192 - 202 ( 11 )
Background: Nifedipine is a potential therapeutic agent for the treatment of cardiovascular disturbances, although it suffers from short half-life (t1/2, 2 hr).
Objective: To address the problem, we first prepared nifedipine loaded sustained release microsponges and then formulated tablets for effective clinical application and patient compliance.
Method: Preparations of microsponges were carried out using different compositions of nifedipine and polymer (1:1, 1:2 and 1:3 % molar ratio) using emulsion solvent diffusion technique.
Results: The microsponges with molar ratio 1:3 (formulation code: MF-3) found optimized as revealed by analyzing surface morphology, better powder flow properties (angle of repose; 28.80 ± 0.9, Hausner ratio 1.15 ± 0.2, % compressibility 15.28 ± 0.5% and higher % drug content (80 ± 1.9 %). Different batches of tablets were then formulated incorporating MF-3 microsponges and different proportions (10-50 %) of microcrystalline cellulose and starch as additives. Among tablet formulations, batch composed of 48% of MF-3, 30% of MCC, 20 % of starch and 2 % of talc (TF-33), showed 92.73 ± 2.19 % drug release during 24 hr in vitro release study in comparison to other batches including commercial formulation which was found to be released completely in 20 hr. Further, stability analysis revealed good drug retention of loaded nifedipine as well as consistent in vitro release pattern over a period of 90 days at 40°C and 75% RH.
Conclusion: The microsponge tablet delivery system was found to be superior concerning the therapeutic advantage as well as manufacturing feasibility of nifedipine.
Cardiovascular diseases, dissolution, drug loading, microsponge drug delivery, microsponge entrapped tablet, nifedipine microsponges, sustained release.
Pharmaceutical Research Lab, Department of Pharmaceutics, BM College of Pharmaceutical Education and Research, Khandwa Road, Indore 452020, Madhya Pradesh, Sri Aurobindo Institute of Pharmacy, Indore-Ujjain State Highway, Near MR-10 Crossing, Indore, TIT College of Pharmacy, Technocrats Institute of Technology Campus, Anand Nagar, Raisen Road, Bhopal, MP- 462021, Pharmaceutical Research Lab, Department of Pharmaceutics, BM College of Pharmaceutical Education and Research, Khandwa Road, Indore 452020, Madhya Pradesh, Discipline of Pharmacy, Graduate School of Health, University of Technology Sydney, Sydney, Ultimo New South Wales 2007, Priority Research Centre for Healthy Lungs, Hunter Medical Research Institute, Lot 1 Kookaburra Circuit, New Lambton Heights, Newcastle, NSW 2305, National Institute of Pharmaceutical Education and Research (NIPER) – Ahmedabad, Department of Pharmaceutics, Opposite Air Force Station Palaj, Gandhinagar, Gujarat 382355