ArticleDrug delivery and translational research2025
Pluronics® F68 and D-α-tocopheryl polyethylene glycol succinate 1000 tailored self-assembled mixed micelles to improve oral bioavailability of oleanolic acid: in vitro and in vivo characterization.
Article in Drug delivery and translational research, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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Abstract
Oleanolic acid (OA) ischaracterized by its low water solubility, poor permeability and majorly metabolized by cytochrome P450 (CYP) isozymes in the intestinal tract, particularly CYP3A, which contribute to the low oral bioavailability. OA has multiple pharmacological actions including hepatoprotective, anti-inflammatory, antidiabetic and antiviral effects. OA classified as a BCS IV drug which have restricted its potential clinical application. In this study D-α-Tocopheryl polyethylene glycol succinate (TPGS) and Pluronics F68 based stabilized OA loaded mixed micellar system (OA-MMs) developed to improve the solubility and permeability. Mixed micelles were characterized by dynamic light scattering studies as a function of temperature, salt addition, and OA solubilisation followed byXRD, FE-SEM and IR analysis confirmed the formation of stabilized OA-MMs with the least size and PDI (10.041 ± 1.35 nm, 0.313 ± 0.012). Scattering studies results demonstrates the formation of stable micelles with no significant alterations insize upon salt addition (up to 150mM NaCl), OA incorporation (up to 150 mM) and temperature rise till 40 °C.Solubility of the pure OA and OA-MMs was found to be 0.042 mg/ml and 1.98 mg/ml. The % cumulative release of drug from alone OA, OA + TPGS and OA-MMs was found to be 4.363 ± 0.025%, 57.18 ± 0.034% and 92.269 ± 0.017% respectively up to 24 h. Single-pass intestinal perfusion studies (SPIP) showed that K
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