274901-16-5 Purity
98%
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Specification
Vancomycin hydrochloride is a water-soluble antibiotic for treating Gram-positive bacterial infections (osteomyelitis, arthritis, endocarditis, pneumonia etc. To enhance therapeutic effectiveness of vancomycin hydrochloride and minimise side-effects (nephrotoxicity in particular), this article invented a chitosan-capped liposome (c-Lips) for administration by intravenous administration of vancomycin hydrochloride (VANH). Injectable c-VANH-Lips could be an attractive vector for VANH for therapeutic targeting Gram-positive bacterial infections and nephrotoxicity.
Preparation procedure of c-VANH-Lips
· The lipid and aqueous fractions were prepared separately. For the lipid phase, 65 mg of soy lecithin and 10 mg of cholesterol were exact measured and mixed in 2 mL of chloroform. The aqueous phase of VANH solution (10 mg/mL) was slowly injected into the lipid phase through a microinjector. It was then sonicated in an ultrasonic bath at room temperature to form a first emulsion.
· Next, the organic solvent was evaporated using a rotary evaporator at 45°C under reduced pressure. To hydrate the mixture, 7.5 mL of distilled water was incorporated and allowed to sit for an additional 5 minutes at controlled temperature. Following this, the liposomal suspension was uniformly dispersed using ultrasound.
· The c-VANH-Lips were subsequently formed through electrostatic deposition, where chitosan was dissolved in 1% acetic acid (v/v) to prepare the chitosan solution. This solution was then diluted with sodium acetate buffer (pH 4.5) and added dropwise to the previously prepared liposome suspension while being stirred magnetically for 30 minutes, resulting in the formation of c-VANH-Lips.
Vancomycin hydrochloride (VH) is very difficult to apply or transmit topically or transdermally, as it has a very high molecular weight and extreme hydrophilicity. This paper examined how permeation enhancers (co- and pre-treatment with chemical permeability enhancers (oleic acid (OA) and palmitic acid (PA)) affected VH permeation through intact and tape-stripped skin.
Evaluation methods and results
It was investigated skin permeation with an excision of porcine skin and a Franz diffusion cell. Continuous anodic iontophoresis was used to boost skin absorption of VH. Pharmacokinetic studies were conducted in Sprague-Dawley rats following topical administration of VH products.
Free VH exhibited negligible skin permeation in the porcine model. However, pharmacokinetic studies revealed that VH could permeate rat skin. Co-treatment of skin with VH and PA resulted in significantly greater permeation enhancement compared to co-treatment with VH and oleic acid (OA). Furthermore, simultaneous application of VH and PA was more effective than sequential application (pre-treating with PA followed by VH). Tape-stripping the skin prior to application of VH and PA further enhanced permeation. A clinically desired plasma concentration of VH was achieved by combining the chemical permeation enhancer PA with skin tape-stripping. While anodic iontophoresis increased VH permeation, it was less effective than the combination of PA and tape-stripping.