Formulation and Evaluation of Anticancer Drug (Tamoxifen) Loaded Nanosponges

Abstract

The purpose of this research was to prepare Tamoxifen loaded Nanosponge gel for Sustained release of drug, increase the drug solubility, and increase the drug permeability, to reduce the dosing frequency and side effects. The FTIR studies proved that there were no interactions between the drug and Polymers. Homogenization technique followed by centrifugation was employed to prepare Nanosponge using various polymers. The formulation were prepared using different Polymers (hydroxy Ethyl cellulose and PVA) in different ratios (Drug: Polymer–1:1, 1:1.5, 1:2, 1:2.5, 1:3, 1:3.5, 1:4 and 1:4.5) Using dichloromethane as cross linker as well as solvent. The formulations were characterized for drug entrapment efficiency. The Drug content of the formulations was observed to be from 62.90 to 95.94. The entrapment efficiency was found to be 68.97 to 99.44. The highest entrapment efficiency was observed with 98.68 and 99.44 for the formulations F4 and F8. The particle size analysis done by Malvern Zeta sizer showed that the average particle size of Tamoxifen loaded Nanosponge F3 average particle size of Tamoxifen loaded Nanosponge is 91.34nm and the poly dispersity index was found to be 0.196 and F8 average particle size of Tamoxifen Nanosponge F7 was 201.34nm and the poly dispersity index was found to be0.178. The in-vitro release of Tamoxifen Nanosponge optimized formulation F4 was found to be 46.39 % and F8was 45.56 % at the end of 24 hours. The drug content of the Gel G1and G2 was found to be 84 % and 81 % respectively. The in-vitro release of Doxorubicin Nanosponge Gel formulation G1 was found to be 28.77% and G2 was 22.12 % at the end of 24hours. The pH of the gels G1 and G2 was found to be 4.98 and 4.82 respectively. The Viscosity of the gels G1 and G2 was found to be 2.839x10 cps and 2.823x10 cps respectively. Both of the optimized formulations of the respected drugs followed first order release kinetics with hi-guchi mechanism. In-vivo test performed showed that the both the formulations of respected drugs able to retain the drug for prolonged periods of time to provide stable drug release and bioavailability