Department of Pharmacognosy, Goa College of Pharmacy, Panaji, Goa University, Goa, India.
PES's Rajaram and Tarabai Bandekar College of Pharmacy, Ponda, Goa University, Goa, India.
PLoS One. 2022 Nov 3;17(11):e0274916. doi: 10.1371/journal.pone.0274916. eCollection 2022.
The present study intends to formulate, characterize and appraise the phospholipid-based nanovesicular system for enhanced delivery of Hesperetin (HT). The quality by design (QbD) approach was employed to prepare Hesperetin naturosomes (HTN) using the solvent evaporation technique and assessed for physicochemical and pharmacological attributes. The FTIR, DSC, and PXRD studies confirmed the successful formation of a vesicular drug-phospholipid complex, while photomicroscopy, SEM, and TEM analysis revealed the morphology of HTN. The functional attributes substantially enhanced the HT's aqueous solubility, drug release, and membrane permeation. The aqueous solubility of HTN was 10-fold more than that of pure HT. Likewise, the in-vitro dissolution data of HTN showed better competence in releasing the HT (>93%) than the pure HT (64%) or the physical mixture (~74%). Furthermore, HTN significantly altered HT permeation (>53%) when compared to pure HT (23%) or the physical mixture (28%). The current study showed that naturosomes are a promising way to improve the solubility in water, bioavailability, and therapeutic effectiveness of drugs.
本研究旨在制备、表征和评价基于磷脂的纳米囊泡系统，以增强橙皮苷（HT）的递送。采用质量源于设计（QbD）方法，使用溶剂蒸发技术制备橙皮苷天然体（HTN），并评估其理化和药理性质。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）研究证实了囊泡药物-磷脂复合物的成功形成，而荧光显微镜、扫描电子显微镜（SEM）和透射电子显微镜（TEM）分析则揭示了 HTN 的形态。功能特性显著提高了 HT 的水溶解度、药物释放和膜透过性。HTN 的水溶解度比纯 HT 高约 10 倍。同样，HTN 的体外溶解数据显示，其释放 HT 的能力（>93%）优于纯 HT（64%）或物理混合物（74%）。此外，与纯 HT（23%）或物理混合物（28%）相比，HTN 显著改变了 HT 的透过率（>53%）。本研究表明，天然体是提高药物水溶性、生物利用度和治疗效果的一种有前途的方法。
