ABSTRACT

Nicardipine belongs to BCS class-II drug having low solubility and orally bioavailability of about 10-40%. The objective of the present study is to develop a nanoparticle based Nicardipine formulation to increase the solubility and dissolution velocity for enhancing the bioavailability while reducing variability in systemic exposure. The obtained ratio of 1:1:1:1 of Drug, chitosan, Hydroxyethyl Beta-Cyclodextrin and cross linking agent sodium tripolyphosphate showing highest solubility of drug in water. The optimized nanoparticles (F3 batch) shown good entrapment efficiency, particle size, poly disparity and zeta potential value. The nanoparticles are filled into a capsule with SSG, Croscarmalose sodium, crospovidone Avicel pH 102 talc and Mg.sterate. The above results indicated crospovidone containing (f12) shown good dissolution and drug content. The Nicardipine Hydrochloride capsules were shown good stability in the studies. The bioavailability studies of Nicardipine nanoparticle based capsules in the rabbit and compared with the pure drug. Nicardipine Nano capsules were shown Cmax68.33 ng/ml, T max at 6 Hr, AUC(0-?) at 191 ng.min/ml and t1/2 at 11.53 hr. AUC and maximum plasma concentration of Nicardipine Nano capsule is higher than pure nicardipine drug it indicates Nicardipine Nano capsules produce more bioavailability than nicardipine hydrochloride. Hence there is no significant difference between the pharmacokinetic parameters of Nicardipine hydrochloride obtained with pure drug and optimized formulation. Thus the prepared Nicardipine Nano capsule proved to be a potential technology for enhancing the transfer of poorly water soluble lipophilic compounds to the aqueous phase, thus enhancing the bioavailability. Keywords: -Nicardipine; Soy PC, DMPC, Aerosil 200, Propylene Glycol, Tween-80
Publication date: 25/09/2021

https://ijbpas.com/pdf/2021/September/MS_IJBPAS_2021_SEPT_SPCL_1031.pdf

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https://doi.org/10.31032/IJBPAS/2021/10.9.1031