Enhancing Hormonal Tablets Disintegration: The Role of Chitosan as an Alternative Disintegrant in Estradiol Tablet Formulation.

Abstract

The vital regulatory role of estradiol in diverse physiological systems, encompassing the menstrual cycle, cardiovascular, neurologic, skeletal, and vascular systems, underscores its importance. Consequently, this compound is frequently incorporated into diverse pharmaceutical formulations, particularly those in tablet form. Typical inactive ingredients used in estradiol tablet formulations include lactose monohydrate, magnesium stearate, microcrystalline cellulose, and sodium starch glycolate. Chitosan, recognized as a novel excipient, is emerging as a promising alternative to microcrystalline cellulose (MCC). In contrast to MCC, chitosan exhibits noteworthy properties, such as excellent solubility in aqueous solutions, a pleasant odor, superdisintegrant effects, increased porosity, and enhanced liquid absorption. The utilization of chitosan as a tablet disintegrant not only enhances tablet bioavailability but also facilitates the formulation of water-soluble tablet formulations and augments cell penetration in nanoparticle chitosan without any chitosan-estradiol interaction. This article will conduct an in-depth examination of the characteristics of chitosan and its disintegration properties, drawing comparisons with those of microcrystalline cellulose. Furthermore, we will investigate potential formulation strategies for the development of effective tablet formulations employing chitosan as a disintegrant. Additionally, attention will be given to several prior studies on the utilization of chitosan as a disintegrant, providing an analysis of their advantages and limitations in diverse pharmaceutical contexts.