Formulation and evaluation of oral mucoadhesive multiparticulate system containing metoprolol tartarate: an in vitro-ex vivo characterization.
The aim of the present study was to prepare mucoadhesive multiparticulate system for oral drug delivery using ionic gelation technique. Microspheres composed of various mucoadhesive polymers including HPMC of various grades like K4M, K15M, K100M, E50LV, Carbopol of grades 971P, 974P and polycarbophil were prepared. In this technique cross linking of sodium alginate with calcium chloride was done which retarded the release of drug from the mucoadhesive polymer. In the present work Metoprolol tararate was used as a model drug. Interaction studies performed using FTIR spectroscopy revealed that there was no drug to polymer interactions. The preliminary mucoadhesive strength studies performed for various polymers using rotating cylindrical method showed that HPMC had greater mucoadhesive properties than carbopol and polycarbophil. Microspheres so prepared were discrete, bulky, free flowing and showed an average encapsulation efficiency ranging from 50-60%. Particle size of the microspheres, as determined by the optical microscopy was found to be between 400-650 microm. The prepared formulations also exhibited a good mucoadhesive strength which was determined in in vitro conditions through falling film technique and was compared with ex vivo studies. The microspheres so prepared also exhibited a good swelling index which confirmed the strong mucoadhesive property of the formulation. Metoprolol release from the multiparticulate system was regulated and extended until 12 hours and exhibited a non fickian drug release kinetics approaching to zero order, as evident from the release rate exponent values which varied between 0.57 to 0.73. The stability studies performed on the optimized batches at 40 degrees C /75% RH for 90 days indicated no significant change in the physicochemical properties.
Belgamwar
Veena
V
R.C. Patel College of Pharmacy, Shirpur, State, Maharashtra, India. veenabelgamwar@yahoomail.com
Shah
Viral
V
Surana
S J
SJ
D000268:Adhesiveness; D000284:Administration, Oral; D000319:Adrenergic beta-Antagonists / Q000737:chemistry*; D000818:Animals; D002626:Chemistry, Pharmaceutical; D016503:Drug Delivery Systems; D004355:Drug Stability; D005782:Gels; D008790:Metoprolol / Q000737:chemistry*; D008863:Microspheres; D051381:Rats; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared
D000319:Adrenergic beta-Antagonists; D005782:Gels; D008790:Metoprolol