A size-switchable microsphere loaded with salmon calcitonin as two-weekly dosing for osteoporosis therapy

IF 4.4 2区 医学 Q1 PHARMACOLOGY & PHARMACY
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Abstract

Osteoporosis is a disease with an increased incidence of fractures due to decreased bone mass and destruction of the microstructure of bone tissue. Salmon calcitonin (sCT), as a peptide, possesses the ability to inhibit osteoclast activity and thus regulate bone metabolism in clinical. However, short half-life and unstable physicochemical properties leading to rapid degradation of sCT have severely limited its clinical application. In this study, a size-switchable microsphere was developed to solve the problem of frequent administration and poor stability of sCT. sCT was encapsulated into Egg PC to form anhydrous reverse micelles (ARM) and then ARM was encapsulated into microspheres (MS@ARM). The degradable composite microspheres were utilized to provide a drug reservoir for sustained release of ARM encapsulated with sCT to reduce the frequency of drug administration, while the released ARM encapsulated with sCT entered the blood circulation to further protect sCT. In vitro release experiments demonstrated that the microspheres could sustain the release of sCT for at least 16 days. The microspheres MS@ARM showed the advanced therapeutic effect on the mouse model of glucocorticoid-induced osteoporosis (GIOP) at a low dosing frequency. The size-switchable microsphere is expected to be a new strategy for delivering sCT for osteoporosis treatment.

Abstract Image

一种装载鲑鱼降钙素的尺寸可调微球,用于骨质疏松症的两周一次给药治疗。
骨质疏松症是一种由于骨量减少和骨组织微结构破坏而导致骨折发生率增加的疾病。鲑鱼降钙素(sCT)作为一种多肽,具有抑制破骨细胞活性的能力,从而在临床上调节骨代谢。然而,sCT 的半衰期短、理化性质不稳定导致其快速降解,严重限制了其临床应用。本研究开发了一种尺寸可调的微球,以解决 sCT 频繁给药和稳定性差的问题。将 sCT 包囊到蛋 PC 中形成无水反向胶束(ARM),然后将 ARM 包囊到微球(MS@ARM)中。这种可降解的复合微球可作为药物储库,用于持续释放包裹有sCT的ARM,以减少给药次数,同时释放的包裹有sCT的ARM进入血液循环,进一步保护sCT。体外释放实验表明,微球可持续释放 sCT 至少 16 天。微球MS@ARM在糖皮质激素诱导的骨质疏松症(GIOP)小鼠模型上显示出了低剂量的先进治疗效果。这种尺寸可调的微球有望成为一种将 sCT 用于骨质疏松症治疗的新策略。
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来源期刊
CiteScore
8.80
自引率
4.10%
发文量
211
审稿时长
36 days
期刊介绍: The European Journal of Pharmaceutics and Biopharmaceutics provides a medium for the publication of novel, innovative and hypothesis-driven research from the areas of Pharmaceutics and Biopharmaceutics. Topics covered include for example: Design and development of drug delivery systems for pharmaceuticals and biopharmaceuticals (small molecules, proteins, nucleic acids) Aspects of manufacturing process design Biomedical aspects of drug product design Strategies and formulations for controlled drug transport across biological barriers Physicochemical aspects of drug product development Novel excipients for drug product design Drug delivery and controlled release systems for systemic and local applications Nanomaterials for therapeutic and diagnostic purposes Advanced therapy medicinal products Medical devices supporting a distinct pharmacological effect.
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