Lyophilized tablets of felodipine-loaded polymeric nanocapsules to enhance aqueous solubility: Formulation and optimization

The aim of this study was to enhance the physicochemical properties of felodipine through the formulation of lyophilized polymeric nanocapsule tablets. Felodipine was loaded into polymeric nanocapsules composed of Labrafac™ PG (an oil solubilizer) and Eudragit® EPO (cationic coating polymer) using the sonoprecipitation technique. The effect of changing quantities of Labrafac™ PG (X₁) and Eudragit® EPO (X₂) on the mean particle size (Y₁), zeta potential (Y₂) and entrapment efficiency (Y₃) were studied via 3² full factorial design.

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Formulation of high loaded polymeric nanocapsules in a quite stable form

Unique incorporation of high loaded polymeric nanocapsules in lyophilized tablets

Lyophilized polymeric nanocapsule tablets prepared by different cryoprotectants

Both factors X₁ and X₂ had a significant effect on the mean particle size, while the zeta potential was affected by X₂. The entrapment efficiency was affected significantly by X₂ and by the interaction between both factors (X₁X₂). After purification by filtration and ultracentrifugation, the optimized formulation was incorporated into lyophilized tablets using poly (vinyl alcohol) as binder and stabilizer and either of two types of cryoprotectant (mannitol or sucrose). Different characterizations were performed on both types of lyophilized polymeric nanocapsule tablets, showing that each type exhibited porous structure, high-level drug content, rapid disintegration, and fast dissolution rate.

Moreover, the saturation solubility for each type was vastly increased. The present study provides a unique formulation of high-level drug-loaded polymeric nanocapsules that could be efficiently incorporated in lyophilized tablets to remarkably enhance its stability and to improve the physicochemical properties of felodipine.

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Article information: Ahmed H. Ibrahim, Hany M. Ibrahim, Ibrahim A. Elbahwy, Mohsen I. Afouna, Tatsuaki Tagami, Tetsuya Ozeki, Lyophilized tablets of felodipine-loaded polymeric nanocapsules to enhance aqueous solubility: Formulation and optimization, Journal of Drug Delivery Science and Technology, 2022. https://doi.org/10.1016/j.jddst.2022.103172.