甲基纤维素湿敏水凝胶中溶菌酶微球性质的体外评价

摘要/Abstract

摘要： Long-term injectable microspheres have some inherent disadvantages such as migration of
micro-spheres from the original site and the burst effect. In order to avoid these
problems, microsphere-loaded thermosen-sitive hydrogel system was designed and expected to
achieve a zero-order release of biomolecular drugs in relative high initial drug loadings.
Lysozyme, an antibacterial protein usually used to reduce prosthetic valve endocarditis,
was selected as the model drug. Poly (DL-lactide-co-glycolide) (PLGA) microspheres,
prepared by solvent evapo-ration method, were employed to encapsulate lysozyme and
dispersed into thermosensitive pre-gel solution con-taining methylcellulose (MC),
polyethylene glycol (PEG), sodium citrate (SC), and sodium alginate (SA). The mix-ture
could act as a drug reservoir by performing sol-gel transition rapidly if the temperature
was raised from room temperature to 37℃. The in vitro release results showed that the
burst effect was avoided due to strengthening of diffusion resistance in the gel. The
formulation was able to deliver lysozyme for over 30 days in a nearly zero-order release
profile with a rate of 32.8μg•d－1 which exhibits its remarkable potential for effective
application in long-term drug delivery.

关键词: microsphere;thermosensitive hydrogel;drug release;lysozyme;methylcellulose

Abstract: Long-term injectable microspheres have some inherent disadvantages such as migration of
micro-spheres from the original site and the burst effect. In order to avoid these
problems, microsphere-loaded thermosen-sitive hydrogel system was designed and expected to
achieve a zero-order release of biomolecular drugs in relative high initial drug loadings.
Lysozyme, an antibacterial protein usually used to reduce prosthetic valve endocarditis,
was selected as the model drug. Poly (DL-lactide-co-glycolide) (PLGA) microspheres,
prepared by solvent evapo-ration method, were employed to encapsulate lysozyme and
dispersed into thermosensitive pre-gel solution con-taining methylcellulose (MC),
polyethylene glycol (PEG), sodium citrate (SC), and sodium alginate (SA). The mix-ture
could act as a drug reservoir by performing sol-gel transition rapidly if the temperature
was raised from room temperature to 37℃. The in vitro release results showed that the
burst effect was avoided due to strengthening of diffusion resistance in the gel. The
formulation was able to deliver lysozyme for over 30 days in a nearly zero-order release
profile with a rate of 32.8μg•d－1 which exhibits its remarkable potential for effective
application in long-term drug delivery.

Key words: microsphere, thermosensitive hydrogel, drug release, lysozyme, methylcellulose

林莹, 孙佳丽, 蒋国强, 昝佳, 丁富新. 甲基纤维素湿敏水凝胶中溶菌酶微球性质的体外评价[J]. CIESC Journal.

LIN Ying, SUN Jiali, JIANG Guoqiang, ZAN Jia, DING Fuxin. In vitro evaluation of lysozyme-loaded microspheres in thermosensitive methylcellulose-
based hydrogel[J]. .

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