Microsponges as Promising Vehicle for Delivery of Antibiotic and Antihistamine for Infectious and Allergic Disorders: Preparation, Characterization and Applications

Abstract

This study is done to achieve the aim of formulating microsponges containing CPM alone and in combination with cefexime as API. The microsponge drug delivery system (MDDS) is a porous polymeric system. These are tiny sponge like particles that consist of myriad of interconnecting voids within a non-collapsible structure with a large porous surface through which active ingredients are released in a controlled manner. In this study microsponges are prepared by using Eudragit RS 100 as polymer and PVA as emulsifying agent in different ratios with constant amount of CPM and cefexime. Quasi emulsion solvent diffusion method was used to formulate microsponges. Percentage yield, percent drug entrapment, flow properties including compressibility by Carr’s index, tapped bulk density, loose bulk density, Haunser’s ratio of these microsponges are calculated. From these studies it was shown that percentage yield increased with the increase in the polymer ratio and percentage entrapment was decreased with the increase in the polymer ratio. Results of Carr’s index and Haunser’s ratio indicate excellent flow properties of all microsponges. These microsponges are then characterized by FT-IR and SEM. In-vitro dissolution studies were carried out in USP dissolution apparatus at 50 rpm at 37±0.5 ͦ C. Release kinetic parameters indicated that formulated optimized microsponges were following the korsmeyer peppas release kinetic. All results of physicochemical parameters and characterization values indicate that the optimized CM9 of CPM containing and CCM9 of CPM-CEF containing microsponge formulations will be good for transforming it further into gels and subjected to different evaluation parameters analysis. Then CPM and CPM-CEF entrapped microsponges loaded gels CMG of CM9 microsponges and CCMG of CCM9 respectively by employing Carbopol as gelling agent and Propylene glycol (PG) and Polyethylene glycol (PEG-1000) as permeation enhancing agent. In-vitro studies were executed with the help of USP dissolution apparatus set at revolutions of 60 rpm and at temperature about 37±0.5 ºC. Release kinetic models depicted that formulated microsponges loaded gel was following the first order release model. In Franz diffusion cells, human skin membrane was used to determine the permeation effects. Fick’s laws were employed to compute permeation kinetic parameters such as Flux (J), Permeation Co-efficient (Kp), Diffusion Co-efficient (D), Enhancement Ratios (ER) and Input Rate (IR) of CMG are done. Preformulation studies of both CMG and CCMG were made through Fourier Transform Infrared spectroscopic (FT-IR) records which illustrated absence of any drug-polymer interactions. All physicochemical distinctive features of gel such as viscosity, solubility, spreadability, mucoadhessive force, extrudibility, homogeneity, pH, partition co-efficient (Ko/w), Draize’s skin irritation test and stability studies at 25±0.5ºC and at 40ºC±0.5ºC were calculated. All results demonstrated that the CMG and CCMG will be favorable for further clinical trials evaluations.