The aim of the present work was to assess the influences of the parameters of the process of preparing polylactide-based nanosomal medicinal formulations of rifampicin (Rif) on nanoparticle size, the level of Rif sorption, and the kinetics of Rif release in vitro. The most effective Rif sorption in nanoparticles (up to 90%) was obtained using polylactides with additional terminal carboxyl groups. An increase in the initial Rif concentration in the organic phase from 1 to 5 mg/ml led to some decrease in the extent of sorption (from 89% to 76%) though it had no significant effect on the sizes of the resulting nanoparticles (190 – 260 nm). The rate of Rif release could be controlled by altering the composition of the polymer matrix of the nanoparticles; the presence of additional terminal carboxyl groups in polylactides gave slower antibiotic release, resulting from tighter interaction with the polymer matrix.
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Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 44, No. 3, pp. 42 – 47, March, 2010.
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Maksimenko, O.O., Vanchugova, L.V., Shipulo, E.V. et al. Effects of technical parameters on the physicochemical properties of rifampicin-containing polylactide nanoparticles. Pharm Chem J 44, 151–156 (2010). https://doi.org/10.1007/s11094-010-0420-y
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DOI: https://doi.org/10.1007/s11094-010-0420-y