Department of Quality Assurance, SVKM's Dr. Bhanuben Nanavati College of Pharmacy, Vile Parle (W), Mumbai, 400 056, India.
Department of Pharmaceutics, Shobhaben Pratapbhai Patel School of Pharmacy & Technology Management, SVKM's NMIMS, Vile Parle (W), Mumbai, 400 056, India.
J Mater Sci Mater Med. 2019 Jun 13;30(6):74. doi: 10.1007/s10856-019-6268-0.
Paliperidone (PLP) is an antipsychotic drug indicated for treatment and management of schizophrenia. The current study demonstrates potential of PLP-loaded β-cyclodextrin-based nanosponges (CDNS) for solubility enhancement and prolonged release of PLP. The inclusion complexes of PLP with carbonyldiimidazole (CDI) cross-linked nanosponges were synthesized. The drug-loaded CDNS were characterized for particle size, zeta potential, encapsulation efficiency, stability study, in vitro drug release studies. The interaction of PLP with CDNS was ascertained by FTIR, DSC and PXRD studies. The particle size and zeta potential values were sufficient to obtain stable formulations. Solubility was significantly increased and in vitro drug release studies revealed prolonged release of PLP from the CDNS for 6 h. PXRD study revealed that the crystallinity of PLP was decreased due to complexation with the CDNS. Thus, cyclodextrin-based nanosponges represent a novel approach for solubility enhancement and improved dissolution of selected model drug PLP.
帕利哌酮（PLP）是一种抗精神病药物，用于治疗和管理精神分裂症。本研究表明，载有帕利哌酮的β-环糊精纳米海绵（CDNS）具有提高溶解度和延长帕利哌酮释放的潜力。用碳二亚胺（CDI）交联纳米海绵合成了帕利哌酮的包合物。对载药 CDNS 进行了粒径、zeta 电位、包封效率、稳定性研究、体外药物释放研究。通过傅里叶变换红外光谱（FTIR）、差示扫描量热法（DSC）和粉末 X 射线衍射（PXRD）研究确定了 PLP 与 CDNS 的相互作用。粒径和 zeta 电位值足以获得稳定的配方。溶解度显著提高，体外药物释放研究表明，PLP 从 CDNS 中释放 6 小时。PXRD 研究表明，由于与 CDNS 的络合，PLP 的结晶度降低。因此，基于环糊精的纳米海绵代表了一种提高所选模型药物 PLP 溶解度和改善溶解的新方法。
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