Chitosan as Valuable Excipient for Oral and Topical Carvedilol Delivery Systems.
Chitosan as Valuable Excipient for Oral and Topical Carvedilol Delivery Systems.
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DOI：
10.3390/ph14080712
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发表时间：
2021-07-23
期刊：
影响因子：
--
通讯作者：
Cielecka-Piontek J
中科院分区：
文献类型：
--
作者：
Sip S;Paczkowska-Walendowska M;Rosiak N;Miklaszewski A;Grabańska-Martyńska K;Samarzewska K;Cielecka-Piontek J
壳聚糖是一种有价值的赋形剂，由于其生物相容性和增加水溶性差的药物的溶解度。本文介绍的研究涉及制备壳聚糖（脱乙酰甲壳素）与卡维地洛（β-受体阻滞剂）的二元组合，以开发具有改良卡维地洛释放曲线的制剂。作为研究的一部分，获得了壳聚糖与卡维地洛的六种物理混合物，并通过光谱（PXRD、FT-IR和拉曼）、热分析（DSC）和显微镜（SEM）方法进行了鉴定。研究的下一阶段估计了卡维地洛在所获得的药物递送系统中的分布变化和溶出速率;参比样品为纯卡维地洛。研究在pH = 1.2和6.8下进行，模拟胃肠道条件。使用开发的等度UHPLC-DAD方法测定卡维地洛的定量变化。建立的表观渗透系数证明了卡维地洛的渗透性的变化后，通过模拟胃肠道和皮肤壁的膜引入药物输送系统。使用体外模型证实了卡维地洛-壳聚糖系统的生物粘附潜力。所进行的研究和获得的结果表明，使用壳聚糖作为赋形剂在现代口服或表皮卡维地洛给药系统的显着潜力。
Chitosan is a valued excipient due to its biocompatibility properties and increasing solubility of poorly water-soluble drugs. The research presented in this paper concerns the preparation of binary combinations of chitosan (deacetylated chitin) with carvedilol (beta-blocker) to develop a formulation with a modified carvedilol release profile. As part of the research, six physical mixtures of chitosan with carvedilol were obtained and identified by spectral (PXRD, FT-IR, and Raman), thermal (DSC), and microscopic (SEM) methods. The next stage of the research estimated the profile changes and the dissolution rate for carvedilol in the obtained drug delivery systems; the reference sample was pure carvedilol. The studies were conducted at pH = 1.2 and 6.8, simulating the gastrointestinal tract conditions. Quantitative changes of carvedilol were determined using the developed isocratic UHPLC-DAD method. Established apparent permeability coefficients proved the changes in carvedilol’s permeability after introducing a drug delivery system through membranes simulating the gastrointestinal tract and skin walls. A bioadhesive potential of carvedilol–chitosan systems was confirmed using the in vitro model. The conducted research and the obtained results indicate a significant potential of using chitosan as an excipient in modern oral or epidermal drug delivery systems of carvedilol.
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