Formulation Development and Evaluation of Injectable Depot Suspension

Abstract

The aim of the present study was to develop sustained release parenteral depot drug delivery system of contraceptive drug (Medroxyprogesteron acetate). Parenteral depots formulations (suspension) are widely used to improve therapeutic value of water insoluble drug’s & provide sustained drug release over a longer duration of time and solve the problem of daily intake of medicine. Long acting hormonal contraceptive depot formulation advanced the practice of contraception, where injectable & subder mal route of administration used. Objective of present study was to develop medroxyprogesteron acetate injectable depot suspension for contraceptive used. Medroxyprogesteron acetate injectable depot suspensions were prepared by sterile combining of API and excipient powders by rapid stirring method. Mixing speed and temperature dependent solubility of parabens were affect the particle size, specific surface area and dissolution rate of given suspension. Different excipients used in the formu lation are Methylparaben & Propyllparaben used as preservative and re-suspending agent, sodium chloride were used Isotonisity modifier, PEG 3350 were used as suspending agent, Tween 80 used as surfactant. The resultant MPA suspension were evaluated for Physical properties, MPA content were 101.00 ± 2 %, viscosity were 8.58 ±1cps, pH 5.826 ±1 and osmolality were found to be 378 ± 5 Mos mol /kg.H2O respectively & further characterized for surface morphology, particle size, zeta potential sedimentation volume, syrengeability, hold time study, In vitro drug release. The suspensions were found to be spherical with smooth surface. Particle size, specific surface area & zeta potential were found to be (Particle size 13.4 µm with specific surface area 1530 cm2/km, -22.66 mV). Interaction be tween the drug and polymer were investigated by Fourier Transform Infrared (FT-IR) Spectroscopy. The MPA injectable suspension could go through 24 gauge hypodermic needle smoothly with withdrawal volume 1.70, mL, MPA suspension re-dispersed within 1 minute without forming clogs. The FT-IR anal ysis confirmed the compatibility of MPA with the excipients without interaction. In- vitro drug release from these MPA injectable suspension showed sustained release over a period of 48 hours (Dissolution type-II apparatus), & 90 minute (Dissolution type- IV apparatus)