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Meloxicam-loaded solvent exchange-induced in situ forming beta-cyclodextrin gel and microparticle for periodontal pocket delivery.
Biomaterials Advances ( IF 5.5 ) Pub Date : 2020-07-08 , DOI: 10.1016/j.msec.2020.111275
Sai Myo Thu Rein 1 , Wai Wai Lwin 2 , Sarun Tuntarawongsa 3 , Thawatchai Phaechamud 4
Affiliation  

The in situ forming system has attracted attention for periodontitis treatment owing to its sustainable drug release localisation at a periodontal pocket. Given its low aqueous solubility, beta-cyclodextrin (β-CD) may serve as a matrix former of solvent exchange-induced in situ forming gel (ISG) and microparticle (ISM). Meloxicam (Mex)-loaded-β-CD ISG and ISM were prepared using β-CD in dimethyl sulphoxide (ISG) as the internal phase and camellia oil comprising 5% glyceryl monostearate as the external phase (ISM). Mex-loaded β-CD systems comprising 40% β-CD were easily injected via a 24-gauge needle. During solvent exchange with phosphate buffer saline (pH 6.8), the highly concentrated β-CD ISG promoted the phase inversion of β-CD aggregates into matrix-like. Upon exposure to aqueous phase, the ISM system comprising 40% β-CD transformed into microparticles and extended the drug release to 7 days with minimised initial burst release following Fickian diffusion. Moreover, the potential degradability was evident from the high weight loss. High maximum deformation force with high viscous character initiated the slow diffusion rate of the solvent from the ISM system. Therefore, 40% β-CD ISM is a potential local Mex-controlled release system of anti-inflammatory drug for periodontitis treatment.



中文翻译:

载有美洛昔康的溶剂交换诱导原位形成β-环糊精凝胶和用于牙周袋递送的微粒。

原位形成系统而备受瞩目在牙周袋,由于其持续药物释放的本地化牙周炎治疗。鉴于其低的水溶性,β-环糊精(β-CD)可作为溶剂交换诱导的原位形成凝胶 ISG 和微粒 ISM)的基质形成剂。以二甲亚砜 ISG 中的β-CD为内相,含有5%单硬脂酸甘油酯的山茶油为外相 ISM ,制备了含美洛昔康 Mex 的β-CD ISG和ISM。。包含40%β-CD的含Mex的β-CD系统很容易通过24号针头注射。在与磷酸盐缓冲液 pH 6.8)进行溶剂交换期间,高浓度的β-CDISG促进了β-CD聚集体相转化为基质状。暴露于水相后,包含40%β-CD的ISM系统转化为微粒,并在Fickian扩散后将药物释放延长至7天,同时初始爆发释放最小。此外,从高重量损失可以看出潜在的可降解性。具有高粘性的高最大变形力引发了溶剂从ISM系统的缓慢扩散。因此,40%的β-CDISM是用于牙周炎治疗的潜在的局部Mex控释抗炎药系统。

更新日期:2020-07-08
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