Formulation and evaluation of multicomponent inclusion complex of cyclosporine A

IF 2.3 4区化学 Q2 Agricultural and Biological Sciences Journal of Inclusion Phenomena and Macrocyclic Chemistry Pub Date : 2024-03-28 DOI:10.1007/s10847-024-01225-5

Sadaf Jamal Gilani, Syed Sarim Imam, Raisuddin Ali

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Abstract

Cyclosporine A (CP) inclusion complex using cyclodextrin (binary) and cyclodextrin with TPGS (ternary) was prepared by the freeze-drying method. The phase solubility study was performed to calculate the solubility parameters. The prepared formulations were evaluated for saturation solubility and drug release studies. The spectroscopy and molecular docking studies were performed to confirm the formation of inclusion complex. The phase solubility results revealed a high stability constant for both binary and ternary samples. A significant enhancement in saturation solubility and dissolution was found in the prepared inclusion complexes. The spectroscopy studies revealed no interaction between the drug and carrier. The molecular docking study displayed the formation of a stable complex with a good docking score. The diffraction pattern showed the conversion of crystalline CP into an amorphous form after the formation of the inclusion complex. The findings were also supported by the saturation solubility study, which showed a significant enhancement in solubility. From the results, it can be concluded that Cyclosporine A inclusion complex using HP βCD with TPGS is an excellent delivery system. Therefore, the prepared delivery systems may be an alternative to the conventional delivery system for enhanced solubility of highly lipophilic drugs.

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环孢素 A 多组分包合物的配制和评估

采用冷冻干燥法制备了使用环糊精（二元）和环糊精与 TPGS（三元）的环孢素 A（CP）包合复合物。进行了相溶解度研究，以计算溶解度参数。对制备的制剂进行了饱和溶解度和药物释放研究。为确认包合物的形成，还进行了光谱和分子对接研究。相溶解度结果显示，二元和三元样品都具有较高的稳定性常数。在制备的包合物中，饱和溶解度和溶解度都有明显提高。光谱研究表明，药物与载体之间没有相互作用。分子对接研究显示形成了稳定的复合物，对接得分良好。衍射图样显示，在形成包合物后，结晶 CP 变成了无定形形式。饱和溶解度研究也证明了这一结论，该研究显示溶解度显著提高。从这些结果中可以得出结论，使用 HP βCD 与 TPGS 的环孢素 A 包合物是一种出色的给药系统。因此，制备的给药系统可以替代传统的给药系统，提高高亲脂性药物的溶解度。

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来源期刊

Journal of Inclusion Phenomena and Macrocyclic Chemistry 化学-化学综合

CiteScore

3.30

自引率

8.70%

发文量

审稿时长

3-8 weeks

期刊介绍： The Journal of Inclusion Phenomena and Macrocyclic Chemistry is the premier interdisciplinary publication reporting on original research into all aspects of host-guest systems. Examples of specific areas of interest are: the preparation and characterization of new hosts and new host-guest systems, especially those involving macrocyclic ligands; crystallographic, spectroscopic, thermodynamic and theoretical studies; applications in chromatography and inclusion polymerization; enzyme modelling; molecular recognition and catalysis by inclusion compounds; intercalates in biological and non-biological systems, cyclodextrin complexes and their applications in the agriculture, flavoring, food and pharmaceutical industries; synthesis, characterization and applications of zeolites. The journal publishes primarily reports of original research and preliminary communications, provided the latter represent a significant advance in the understanding of inclusion science. Critical reviews dealing with recent advances in the field are a periodic feature of the journal.