期刊
JOURNAL OF PHARMACEUTICAL SCIENCES
卷 111, 期 8, 页码 2322-2329出版社
ELSEVIER SCIENCE INC
DOI: 10.1016/j.xphs.2022.03.008
关键词
Muscle(s); Polylactic acid (PLA); Polyglycolic acid (PLGA); Microsphere(s); Controlled release; Long-acting
资金
- Astellas Pharma Inc.
This study developed a sustained release testosterone formulation for the treatment of fecal incontinence. The formulation effectively affected both the internal and external anal sphincters with a sufficient safety profile.
The objective of this study was to develop a testosterone sustained release formulation for the treatment of fecal incontinence. To suppress the initial burst release of testosterone, which can lead to systemic toxicity, we incorporated a washing step using an aminoalkyl methacrylate copolymer E solution or propylene glycol solution into a typical o/w emulsion method to prepare polylactic-co-glycolic acid microspheres. We used this method to develop a polylactic-co-glycolic acid microsphere formulation that shows sustained release of testosterone for up to one month. Not only did this formulation show a sustained release profile after administration into the intersphincteric groove in minipigs, it also increased both the anal pressure and mass of the external anal sphincter, while keeping systemic testosterone exposure low. Thus, this formulation successfully affected both the internal and external anal sphincters with a sufficient safety profile, deeming it a promising candidate treatment strategy for fecal incontinence. (c) 2022 American Pharmacists Association. Published by Elsevier Inc. All rights reserved.
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