Polymers Enhance Chlortetracycline Hydrochloride Solubility

• Published in: International journal of molecular sciences Vol. 25; no. 19; p. 10591
• Main Authors: Zhang, Chao, Li, Bing, Bai, Yubin, Liu, Yangling, Zhang, Yong, Zhang, Jiyu
• Format: Journal Article
• Language: English
• Published: Switzerland MDPI AG 01.10.2024; MDPI
• Subjects: 2-Hydroxypropyl-beta-cyclodextrin - chemistry; Analysis; Anti-Bacterial Agents - chemistry; Bioavailability; Calorimetry, Differential Scanning; Chlortetracycline; Chlortetracycline - chemistry; chlortetracycline hydrochloride; Crystallization; Dissolution; Drug Carriers - chemistry; Drug delivery systems; Drug dosages; Drugs; Evaluation; gelatin; Gelatin - chemistry; Humidity; hydroxypropyl-β-cyclodextrin; Morphology; Particle Size; Polymer industry; Polymers; Polymers - chemistry; Povidone - chemistry; povidone K30; Ratios; Scanning electron microscopy; solid dispersion; Solubility; Spectroscopy, Fourier Transform Infrared; Thermogravimetry; Vehicles; X-Ray Diffraction; China; solid dispersion; povidone K30; hydroxypropyl-β-cyclodextrin; solubility; chlortetracycline hydrochloride; characterization; gelatin
• ISSN: 1422-0067; 1661-6596; 1422-0067
• DOI: 10.3390/ijms251910591

Chlortetracycline hydrochloride (CTC) is a broad-spectrum tetracycline antibiotic with a wide range of antibacterial activities. Due to low solubility, poor stability, and low bioavailability, clinical preparation development is limited. We sought to improve these solubility and dissolution rates by preparing solid dispersions. A hydrophilic polymer was selected as the carrier, and a solid dispersion was prepared using a medium grinding method, with samples characterized by scanning electron microscopy (SEM), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), powder X-ray diffraction (PXRD), Fourier-transform infrared spectroscopy (FT-IR), and particle size distribution (PSD). To maximize CTC solubility and stability, different polymer types and optimal drug-to-polymer ratios were screened. The solubility of optimized povidone K30 (PVPK30) (1/0.75, / )-, hydroxypropyl-β-cyclodextrin (HP-β-CD) (1/2, / )-, and gelatin (1/1, / )-based solid dispersions was 6.25-, 7.7-, and 3.75-fold higher than that of pure CTC powder, respectively. Additionally, in vitro dissolution studies showed that the gelatin-based solid dispersion had a higher initial dissolution rate. SEM and PS analyses confirmed that this dispersion had smaller and more uniform particles than PVPK30 and HP-β-CD dispersions. Therefore, successful solid polymer dispersion preparations improved the CTC solubility, dissolution rates, and stability, which may have potential as drug delivery systems.