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Int. J. Mol. Sci. 2016, 17(9), 1546; doi:10.3390/ijms17091546

Preparation and Evaluation of Enteric-Coated Chitosan Derivative-Based Microparticles Loaded with Salmon Calcitonin as an Oral Delivery System

Department of Drug Delivery Research, Hoshi University, 2-4-41 Ebara, Shinagawa-ku, Tokyo 142-8501, Japan
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Author to whom correspondence should be addressed.
Academic Editor: Hitoshi Sashiwa
Received: 7 June 2016 / Revised: 29 August 2016 / Accepted: 6 September 2016 / Published: 13 September 2016
(This article belongs to the Special Issue Chitins 2016)
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Abstract

Background: The production of protein drugs has recently increased due to advances in biotechnology, but their clinical use is generally limited to parenteral administration due to low absorption in non-parenteral administration. Therefore, non-parenteral delivery systems allowing sufficient absorption draw much attention. Methods: Microparticles (MP) were prepared using chitosan-4-thio-butylamidine conjugate (Ch-TBA), trimethyl-chitosan (TMC), and chitosan (Ch). Using salmon calcitonin (sCT) as a model protein drug, Ch-TBA-, Ch-TBA/TMC (4/1)-, and Ch-based MP were produced, and their Eudragit L100 (Eud)-coated MP, named Ch-TBA-MP/Eud, Ch-TBA/TMC-MP/Eud, and Ch-MP/Eud, respectively, were prepared as oral delivery systems. These enteric-coated microparticles were examined in vitro and in vivo. Results: All microparticles before and after enteric coating had a submicron size (600–800 nm) and micrometer size (1300–1500 nm), respectively. In vitro release patterns were similar among all microparticles; release occurred gradually, and the release rate was slower at pH 1.2 than at pH 6.8. In oral ingestion, Ch-TBA-MP/Eud suppressed plasma Ca levels most effectively among the microparticles tested. The relative effectiveness of Ch-TBA-MP/Eud to the intramuscular injection was 8.6%, while the sCT solution showed no effectiveness. Conclusion: The results suggest that Eud-coated Ch-TBA-based microparticles should have potential as an oral delivery system of protein drugs. View Full-Text
Keywords: chitosan-4-thio-butylamidine conjugate microparticles; Eudragit L100-coated microparticles; salmon calcitonin; particle feature; in vitro release; in vivo efficacy; oral drug delivery system chitosan-4-thio-butylamidine conjugate microparticles; Eudragit L100-coated microparticles; salmon calcitonin; particle feature; in vitro release; in vivo efficacy; oral drug delivery system
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MDPI and ACS Style

Onishi, H.; Tokuyasu, A. Preparation and Evaluation of Enteric-Coated Chitosan Derivative-Based Microparticles Loaded with Salmon Calcitonin as an Oral Delivery System. Int. J. Mol. Sci. 2016, 17, 1546.

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