Abstract
Objective: The purpose of this research work is to formulate and optimize mucoadhesive microspheres of nifedipine using Carbopol 934P as mucoadhesive and ethyl cellulose as a carrier polymer for controlling the release of nifedipine.
 Methods: The emulsion solvent evaporation technique was used for the preparation of microspheres and the 32 full factorial designs were employed for optimization of microspheres. The developed microspheres were characterized for percent yield, entrapment efficiency, particle size, in vitro release study, percent mucoadhesion, surface morphology, and stability study.
 Results: Evaluating outcomes of preliminary batches indicated that 100 ml volume of processing medium, 5 h stirring time and 2% concentration of emulsifying agent were suitable for spherical, free-flowing microspheres and high percentage drug entrapment efficiency. The optimized batch exhibited 84.35% drug entrapment efficiency, 61.78% mucoadhesion and drug release were also sustained for more than 12 h. Scanning electron microscopy study revealed that produced microspheres were spherical in shape.
 Conclusion: Experimental responses of the optimized batch have close proximity with the predicted value and stability study of the optimized formulation proved the formulation is stable for a long period of time; hence, it is an excellent alternative over the conventional delivery system.
Highlights
IntroductionNifedipine [Dimethyl 1,4–dihydro–2,6–dimethyl–4-(2-nitrophenyl) pyridine–3,5–dicarboxylate] is one of the drugs which is most effective and extensively used in the management of angina (especially in Prinzmetal’s angina) and hypertension
Nifedipine [Dimethyl 1,4–dihydro–2,6–dimethyl–4-(2-nitrophenyl) pyridine–3,5–dicarboxylate] is one of the drugs which is most effective and extensively used in the management of angina and hypertension
Preliminary batches C1 to C12 were prepared to study the effect of the concentration of emulsifying agents and stirring time on the percent yield, particle size, drug entrapment efficiency, mucoadhesion, and shape of the microspheres
Summary
Nifedipine [Dimethyl 1,4–dihydro–2,6–dimethyl–4-(2-nitrophenyl) pyridine–3,5–dicarboxylate] is one of the drugs which is most effective and extensively used in the management of angina (especially in Prinzmetal’s angina) and hypertension. For the enhancement of bioavailability of the drug, it facilitates the intimate contact of the dosage form with the underlying absorption surface [8]. The interactions of bioadhesive polymers to the mucin layer of the mucous membrane are referred to as mucoadhesion [9]. It can be achieved by the specific and nonspecific interaction of bioadhesive polymer with a mucus layer [10]. The adhesion of microspheres with a mucus layer achieved by two stages, first wetting of the microspheres after that, the establishment of adhesive interaction [13,14]
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