Porous and highly responsive cross-linked β-cyclodextrin based nanomatrices for improvement in drug dissolution and absorption

• Published in: Life sciences (1973) Vol. 267; p. 118931
• Main Authors: Badshah, Syed Faisal, Akhtar, Naveed, Minhas, Muhammad Usman, Khan, Kifayat Ullah, Khan, Samiullah, Abdullah, Orva, Naeem, Abid
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier Inc 15.02.2021; Elsevier BV
• Subjects: Animals; beta-Cyclodextrins - chemistry; Biocompatibility; Calorimetry, Differential Scanning; Chlorthalidone; Chlorthalidone - chemistry; Chlorthalidone - pharmacology; Constituents; Crosslinking; Cyclodextrins; Drug Delivery Systems - methods; Drug Liberation - physiology; Fourier transforms; Free radical polymerization; Free radicals; Functional groups; Infrared spectroscopy; Male; Microscopy, Electron, Scanning; Morphology; Nanomatrices; Nanomedicine - methods; Particle Size; Poor solubility; Porosity; Rabbits; Solubility; Solubility - drug effects; Spectroscopy, Fourier Transform Infrared - methods; Spectrum analysis; Toxicity; X-Ray Diffraction; β-Cyclodextrin; Poor solubility; β-Cyclodextrin; Chlorthalidone; Nanomatrices
• ISSN: 0024-3205; 1879-0631
• DOI: 10.1016/j.lfs.2020.118931

Aim of the study was to enhance the solubility of Chlorthalidone by developing beta-cyclodextrin cross-linked hydrophilic nanomatrices. Nine different formulations were fabricated by free radical polymerization technique. All formulations were characterized through different studies. FTIR spectroscopy of unloaded and loaded nanomatrices was processed to determine compatibility of constituents and that of the drug with the system. Surface morphology of the nanomatrices was studied by SEM. The size of the optimized formulation was determined by zeta sizer. Swelling, in-vitro release and solubility studies were carried out in different media and results of in-vitro release profiles of nanomatrices and commercially available tablet of Chlorthalidone were compared. For determination of biocompatibility, toxicity studies were proclaimed in rabbits. Main peaks of corresponding functional groups of individual constituents and that of drug were depicted in FTIR spectra of unloaded and loaded nanomatrices. Porous and fluffy structure was visualized through SEM images. Particle size of the optimized formulation was in the range of 175 ± 5.27 nm. Percent loading of optimized formulation showed the best result. Comparing the in-vitro drug release profiles of nanomatrices and commercially available tablet, the results of the synthesized nanomatrices were quite satisfactory. Solubility profiles were also high as compared to the drug alone. Moreover, toxicity studies confirmed that nanomatrices were biocompatible and no sign of any toxic effect was found. We concluded that our developed nanomatrices had successfully enhanced the solubility of Chlorthalidone and can also be used for other poorly aqueous soluble drugs. [Display omitted]