Smriti Khatri
RamEesh Institute of Vocational and Technical Education, India
Title: Designing Development and evaluation of Floating Gastroretentive Microspheres of Acyclovir with piperine as a bioenhancer
Biography
Biography: Smriti Khatri
Abstract
Introduction: Acyclovir is an effective antiviral drug for the treatment of Herpes simplex virus. Oral bioavailability of Acyclovir is poor (15-20 %) because of low solubility and short half life. Piperine enhances the bioavailability of Acyclovir by increasing the absorption and by delaying the metabolism of the drug. Floating microspheres are prepared to retain the dosage form at the site of absorption and thus enhance the bioavailability. These are low-density system, which are having a sufficient buoyancy to float over the gastric contents and remain in the stomach for a prolonged period. While the system floats over the gastric content, the drug is released slowly at the desired rate. It results in increased gastroretentive time and reduces fluctuation in the plasma drug concentration. Methods: Ethyl cellulose and HPMCK4M were used as polymers for preparing microspheres and piperine was added as a bioenhancer to increase the bioavailability. The microspheres were characterized with respect to their morphology, particle size, encapsulation efficiency, production yield, in-vitro release and pharmacokinetic studies in rats. Result and discussion: The mean particle size was within range and showed spherical shape. Microspheres were having sufficient entrapment efficiency and floating ability and were directly proportional to the polymer concentration. Pharmacokinetic study in rats showed nearly two times higher AUC value of acyclovir for the microspheres with piperine (15614.13±6953.13 ng h/ml) as compared to drug solution (7552.33±3219.09 ng h/ml). In addition, Acyclovir microspheres showed the ability to maintain the acyclovir plasma concentration through 24 h.