Electrospun hydroxypropyl methyl cellulose phthalate (HPMCP)/erythromycin fibers for targeted release in intestine

Abstract

Ultrafine fiber mats of hydroxypropyl methyl cellulose phthalate (HPMCP) were successfully electrospun and explored as drug delivery vehicles using erythromycin as a model drug. The morphology of the electrospun fiber and the drug release process in the artificial gastric juice and in the artificial intestinal juice were investigated. With the same drug-to-matrix ratio (HPMCP/erythromycin ¼ 9/1), all the fibers were electrospun into a tape-like or ribbon shape and the average fiber diameter (AFD) was increased with the HPMCP concentration. Because of the pH-sensitive property of HPMCP, erythromycin was released from the erythromycin-containing electrospun HPMCP fiber mats by a slowly diffusion process in the artificial gastric juice, while it was released in nearly first-order kinetics in the artificial intestinal juice because of the first-order kinetics dissolution of the HPMCP fibers in the artificial intestinal juice. And the rate of erythromycin released in the artificial intestinal juice was about more than 2.5 times faster than that in the artificial gastric juice. The diameter of the fibers plays an important role on the rate and the total amount of the drug released both in stomach and in intestine, the rate and the total amount of the drug released decreasing with increasing AFD.

Applications of electrospun nanofibers

“…Non-biodegradable polymers, such as PEU [194] , were also investigated. Model drugs that have been studied include water soluble [180,183,185] , poor-water soluble [192,[194][195][196][197][198] and waterinsoluble drugs [181,184,199,200] . The release of macro-molecules, such as DNA [187] and bioactive proteins [193,[201][202][203][204] , from nanofibers was also investigated.…”

Drug delivery systems using biotextiles

“…This might be employed advantageously in the preparation of colon-targeted DDSs. 53 Other types of polymers, such as those degradable by microbial enzymes in the colon, might also be used for colon-targeted DDSs. Polymers forming fi rm layers and polymers with bio adhesive properties may also be incorporated into fi lament-forming materials for the preparation of colon-targeted biotextiles.…”

Effects of thermal and chemical treatments on the structural stability of cellulose acetate nanofibers

“…To enhance the solubility of cellulose and hence its electrospinnability, cellulose derivatives have been extensively exploited (Frenot, Henriksson, & Walkenstrom, 2007;S.O. Han et al, 2008;Han, Son, Youk, Lee, & Park, 2005; S. Liu & Hsieh, 2003;Park, Han, & Lee, 2007;Son, Youk, Lee, & Park, 2004;Tungprapa et al, 2007;Wang, Wang, & Huang, 2007;Wu, Wang, Yu, & Huang, 2005;Zhao, Wu, Wang, & Huang, 2003; & Huang, 2004). Among these derivatives, cellulose acetate was used in different solvent systems to produces nanofibers that were then converted to cellulose by de-acetylation (Chen, Bromberg, Hatton, & Rutledge, 2008;Liu & Hsieh, 2002;Lu & Hsieh, 2009;Ma & Ramakrishna, 2008;Ritcharoen, Supsphol, & Pavsdsnt, 2008;Yoon, Moon, Lyoo, Lee, & Park, 2009;Zhao et al, 2003).…”