Abstract
In recent years, the world has faced the issue of antibiotic resistance. Methicillin-resistant Staphylococcus aureus (MRSA) is a significant problem in various treatments and control of infections. Biocompatible materials with saturated fatty acids of different chain lengths (C8–C18) were studied as matrix formers of localized injectable vancomycin HCl (VCM)-loaded antisolvent-induced in situ forming matrices. The series of fatty acid-based in situ forming matrices showed a low viscosity (5.47–13.97 cPs) and pH value in the range of 5.16–6.78, with high injectability through a 27-G needle (1.55–3.12 N). The preparations exhibited low tolerance to high concentrations of KH2PO4 solution (1.88–5.42% v/v) and depicted an electrical potential change during phase transformation. Their phase transition and matrix formation at the microscopic and macroscopic levels depended on the chain length of fatty acids and solvent characteristics. The VCM release pattern depended on the nucleation/crystallization and solvent exchange behaviors of the delivery system. The 35% w/v of C12–C16 fatty acid-based in situ forming matrix prolonged the VCM release over seven days in which C12, C14, C16 –based formulation reached 56, 84, and 85% cumulative drug release at 7th day. The release data fitted well with Higuchi’s model. The developed formulations presented efficient antimicrobial activities against standard S. aureus, MRSA, Escherichia coli, and Candida albicans. Hence, VCM-loaded antisolvent-induced fatty acid-based in situ forming matrix is a potential local delivery system for the treatment of local Gram-positive infection sites, such as joints, eyes, dermis of surgery sites, etc., in the future.
Highlights
The in situ forming system has emerged as a useful drug delivery system owing to its unique behavior of self-transformation at the target site
Caprylic acid (CPL) (≥99%, Batch No 289D1190515A), capric acid (CPR) (≥99%, Batch No 219D161222A), lauric acid (LAU) (≥99%, Batch No 229F170S08A), myristic acid (MYR) (≥99%, Batch No FPLK437 × 4S), and palmitic acid (PAL) (≥99%, Batch No 668F180902D), which were procured from Pacific Oleochemicals, Pasir Gudang, Malaysia, and stearic acid (STR) (≥98, Batch No 3452018), which was purchased from CT Chemical, Bangkok, Thailand, were used as matrix formers
The hydrophobicity of long hydrocarbon chains can dominate the acidity of the carboxyl group, and long-chain fatty acids have high pK values [48,49], which results in the low protonation of fatty acids [50]
Summary
The in situ forming system has emerged as a useful drug delivery system owing to its unique behavior of self-transformation at the target site. Fatty acids are synthesized/metabolized in the human body and found in our food [15,16,17,18]; they are known for their biocompatible and inert properties [18,19]. They have been widely used in the pharmaceutical and cosmetical fields [20,21]. Six saturated fatty acids that carry 8–18 carbon atoms were selected to be studied as core components for fatty acid-based in situ forming matrix in this investigation. Caprylic acid (CPL), capric acid (CPR), lauric acid (LAU), myristic acid (MYR), palmitic acid (PAL), and stearic acid (STR) were used as the matrix formers
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