Department of Pharmaceutics, Faculty of Pharmacy, The Islamia University of Bahawalpur, Bahawalpur, Punjab, Pakistan.
College of Pharmacy, University of Sargodha, Sargodha, Pakistan.
Drug Dev Ind Pharm. 2021 Mar;47(3):465-476. doi: 10.1080/03639045.2021.1892738. Epub 2021 Mar 2.
Poor solubility is an ongoing issue and the graph of poorly soluble drugs has increased markedly which critically affect their dissolution, bioavailability, and clinical effects. This common issue needs to be addressed, for this purpose a series of polyethylene glycol (PEG-4000) based nanogels were developed by free radical polymerization technique to enhance the solubility, dissolution, and bioavailability of poorly soluble drug meloxicam (MLX), as improved solubility is the significant application of nanosystems. Developed nanogels formulations were characterized by FTIR, XRD, SEM, zeta sizer, percent equilibrium swelling, drug loaded content (DLC), drug entrapment efficiency (DEE), solubility studies, and dissolution studies. Furthermore, cytotoxicity studies were conducted in order to determine the bio-compatibility of the nanogels drug delivery system to biological environment. Nanogels particle size was found to be 156.19 ± 09.33 d.nm. Solubility study confirmed that the solubility of poorly soluble drug MLX was significantly enhanced up to 36 folds as compared to reference product (Mobic). The toxicity study conducted on rabbits and MTT assay endorsed the safety of the developed nanogels formulations to the biological system.
溶解度差是一个持续存在的问题，溶解度差的药物的图谱显著增加，这严重影响了它们的溶解、生物利用度和临床效果。为了解决这个常见的问题，我们采用自由基聚合技术开发了一系列基于聚乙二醇（PEG-4000）的纳米凝胶，以提高溶解度差的药物美洛昔康（MLX）的溶解度、溶解和生物利用度，因为提高溶解度是纳米系统的重要应用。所开发的纳米凝胶制剂通过傅里叶变换红外光谱（FTIR）、X 射线衍射（XRD）、扫描电子显微镜（SEM）、Zeta 粒径仪、平衡溶胀度百分比、载药量（DLC）、包封效率（DEE）、溶解度研究和溶出度研究进行了表征。此外，还进行了细胞毒性研究，以确定纳米凝胶药物传递系统对生物环境的生物相容性。纳米凝胶的粒径被发现为 156.19±09.33 d.nm。溶解度研究证实，与参比产品（Mobic）相比，溶解度差的药物 MLX 的溶解度显著提高了 36 倍。在兔子身上进行的毒性研究和 MTT 分析都证实了所开发的纳米凝胶制剂对生物系统的安全性。
