Preparation and quality evaluation of sustained-release microspheres loaded with vancomycin
Objective To prepare stable,safe,and effective vancomycin sustained-release microspheres and evaluate their quality characteristics.Methods Vancomycin microspheres were prepared by mixing polylactic acid(PLA)and poly(lactic-co-glycolic acid)(PLGA)in three different proportions by solvent volatilization method.The effects of different concentrations of polyvinyl alcohol(PVA),the ratio of internal water phase to external water phase on size,encapsulation rate,and drug loading of the microspheres were studied by single factor experiment,and the optimal PLA/PLGA sustained-release microspheres loaded with vancomycin were prepared.The pharmacodynamics of methicillin-resistant Staphylococcus aureus(MRSA)were studied in vivo and in vitro.One-way analysis of variance was used.Results The concentration of PVA and ratio of internal water phase to external water phase had little effect on the encapsulation rate and drug loading of vancomycin(P＞0.05),but the mass ratio of PLA and PLGA in microspheres had significant effects on the encapsulation rate and drug loading of vancomycin(P＜0.000 1).The microsphere size(41.95 μm),encapsulation rate[(28.87±0.32)％],and drug loading[(17.80±0.21)％]were the largest when PLA was pure.The antibacterial activity of vancomycin microspheres against MRSA 252 was higher than that of aqueous solution(0.391 ng/L vs.0.781 ng/L)(P＜0.000 1).Vancomycin microspheres showed more satisfactory bactericidal activity in the treatment of MRSA 252 than vancomycin aqueous solution with the same concentration(P＜0.05).The wound healing effect of vancomycin microspheres on MRSA 252 infected mice was better than that of vancomycin aqueous solution.Conclusions The prepared PLA/PLGA sustained release microspheres can achieve local controlled release of vancomycin drug by adjusting the proportion of PLA and PLGA in the blend to improve drug encapsulation rate and drug loading,tailor degradation rate and change drug release,which is an effective preparation against Staphylococcus aureus infection.
万方数据
维普
