SRES' Sanjivani College of Pharmaceutical Education & Research Kopargaon, Ahmednagar, Maharashtra 423 603, India; J.N.T. University, Hyderabad, 500 085, India.
PES' Modern College of Pharmacy, Yamunanagar, Sector 21, Nigdi, Pune, Maharashtra 411 044, India.
Eur J Pharm Biopharm. 2018 May;126:177-186. doi: 10.1016/j.ejpb.2017.06.024. Epub 2017 Jun 24.
Bosentan is a dual endothelin receptor antagonist used in the treatment of pulmonary arterial hypertension (PAH). But the solubility and bioavailability of this drug are poor, which has restricted the design and development of dosage forms for efficient and successful therapy. The present study was carried out to develop nanocomposites using an amphiphilic graft co-polymer (Soluplus®) as a carrier to enhance the solubility and bioavailability of bosentan. The graft co-polymer-based nanocomposite formulation was prepared using the single-emulsion technique. The nanocomposite was characterised in terms of particle size analysis, solubility, percentage entrapment efficiency, drug-loading capacity, surface morphology, drug content, in vitro dissolution, stability and bioavailability. FT-IR study revealed that there was no interaction between the drug and Soluplus®. DSC analysis of the nanocomposite formulation confirmed that the bosentan was completely encapsulated within a Soluplus®. XRD analysis showed that the drug was converted to an amorphous form irreversibly. SEM images showed that the particles were of size 96-129μm and had slightly smooth to rough textured surface. TEM analysis indicated that the diameters of the prepared bosentan nanocomposite after dispersion in distilled water were 13.69-96.78nm. Statistically significant increases in the solubility, dissolution and bioavailability of the drug were observed. It was confirmed that the use of a graft co-polymer carrier-based nanocomposite formulation is a good approach for efficient delivery of bosentan, the solubility and bioavailability being increased manifold.
波生坦是一种用于治疗肺动脉高压（PAH）的双重内皮素受体拮抗剂。但是，该药物的溶解度和生物利用度较差，这限制了高效和成功治疗的剂型设计和开发。本研究旨在开发纳米复合材料，使用两亲性接枝共聚物（Soluplus®）作为载体来提高波生坦的溶解度和生物利用度。使用单乳液技术制备接枝共聚物基纳米复合材料制剂。对纳米复合材料进行了粒径分析、溶解度、包封效率百分比、载药量、表面形态、药物含量、体外溶出度、稳定性和生物利用度等方面的表征。FT-IR 研究表明药物与 Soluplus®之间没有相互作用。纳米复合材料制剂的 DSC 分析证实波生坦完全被包封在 Soluplus®内。XRD 分析表明药物不可逆地转化为无定形形式。SEM 图像显示，颗粒尺寸为 96-129μm，表面略有光滑至粗糙纹理。TEM 分析表明，在蒸馏水中分散后制备的波生坦纳米复合材料的直径为 13.69-96.78nm。观察到药物的溶解度、溶解和生物利用度有显著增加。证实使用接枝共聚物载体基纳米复合材料制剂是提高波生坦有效传递的一种很好的方法，其溶解度和生物利用度大大提高。
