A novel approach in mucoadhesive drug delivery system to improve zidovudine intestinal permeability

Abstract

Zidovudine (AZT) mucoadhesive solid dispersions (SD) were prepared using a sodium starch glycolate (SSG) and hypromellose phthalate (HPMCP) mixtures as carrier to enhance the intestinal permeability and bioavailability of zidovudine. SDs were prepared using the co-precipitation method followed by solvent evaporation and characterized according to their physicochemical properties such as particle size, crystallinity, thermal behavior, and liquid uptake ability. In vitro drug dissolution, mucoadhesiveness and AZT intestinal permeability were also determined. Thermal behavior and X-ray diffraction patterns demonstrated the amorphous state of AZT in SD systems. The HPMCP polymer restricted the liquid uptake ability in the acid medium; however, this property significantly increased with higher pH values. SDs allowed drug dissolution to occur in a controlled manner. HPMCP decreased the dissolution rates in the acid medium. The mucoadhesiveness of SDs was demonstrated and the permeability of AZT carried in solid dispersions was significantly improved. The effect of the SD carrier polymers on blocking efflux pump can be an important approach to improve the bioavailability of AZT.Uniterms: Zidovudine. Solid dispersion. Mucoadhesion. P-glycoprotein. Intestinal permeability.

Thermoresponsive Azithromycin-Loaded Niosome Gel Based on Poloxamer 407 and Hyaluronic Interactions for Periodontitis Treatment

“…Therefore, the obtained molecular structure was loosely packed and combined with low textural hardness, and was also prone to erosion. Moreover, AGZ8’s high mucoadhesion also contributed to the high permeation rate due to its formation of a strong mucoadhesive interface, which adhered closer to the mucous [ 49 ]. When making comparisons between AZG3, 6, and 9, which had equivalent amounts of HA (2%), AZG9 with 19% of P407 showed the highest permeation rate, followed by 6 (18% of P407) and 3 (17% of P407).…”

Untitled

“…27 Drug targeting colon is used for the treatment of diseases like inflammatory bowel disease, amoebiasis, colonic cancer, ulcerative colitis, Crohn's disease, etc. 28 Intestinal mucoadhesive drug delivery system increases the residence time of the dosage form at the targeted site and facilitates absorption that contributes to improved therapeutic performance 29 . Drugs showing narrow therapeutic index are highly effective if targeted to the desired site of the GIT 30 .…”