Sayed, S., B. A. Habib, and G. M. Elsayed, "Tri-block co-polymer nanocarriers for enhancement of oral delivery of felodipine: preparation, in vitro characterization and ex vivo permeation", Journal of Liposome research, pp. 1-11, 2017. Abstracttri.docx

This study aimed to prepare, optimize and characterize novel felodipine-loaded polymeric
nanomicelles, using a pluronic mixture of F127 and P123. Thin-film hydration method was
adopted for the preparation of different polymeric nanomicelles (T1–T12) according to a 41.31
full factorial design. Factors studied were: Pluronic_:drug ratio (P:D ratio) (10, 20, 30 and
40 w/w) and percent of hydrophilic polymer (F127%) (33.33%, 50% and 66.67% w/w).
Optimization criteria were to maximize transmittance percent (T%) and entrapment efficiency
percent (EE%) and to minimize particle size (PS) and polydispersity index (PDI). The optimized
formulation was further characterized by DSC, FTIR and 1H NMR studies. It was also subjected to
stability testing and ex vivo permeation using rabbit intestines. Spherical nanomicelles of
particle size ranging from 26.18 to 87.54nm were successfully obtained. The optimized
formulation was found to be the already prepared formulation T12 (P:D ratio of 40 and 66.67%
F127) with suitable T% and EE% of 95.12% and 91.75%, respectively. DSC, FTIR and 1H NMR
studies revealed felodipine (FLD) incorporation within T12 nanomicelles. T12 enhanced the
ex vivo intestinal permeation of FLD when compared to a drug suspension and showed good
stability. Therefore, pluronic nanomicelles could be promising for improved oral delivery of FLD.

Habib, B. A., and M. H. H. AbouGhaly, "Combined mixture-process variable approach: a suitable statistical tool for nanovesicular systems optimization.", Expert opinion on drug delivery, vol. 13, issue 6, pp. 777-88, 2016 Jun. Abstract

OBJECTIVES: This study aims to illustrate the applicability of combined mixture-process variable (MPV) design and modeling for optimization of nanovesicular systems.

METHODS: The D-optimal experimental plan studied the influence of three mixture components (MCs) and two process variables (PVs) on lercanidipine transfersomes. The MCs were phosphatidylcholine (A), sodium glycocholate (B) and lercanidipine hydrochloride (C), while the PVs were glycerol amount in the hydration mixture (D) and sonication time (E). The studied responses were Y1: particle size, Y2: zeta potential and Y3: entrapment efficiency percent (EE%). Polynomial equations were used to study the influence of MCs and PVs on each response. Response surface methodology and multiple response optimization were applied to optimize the formulation with the goals of minimizing Y1 and maximizing Y2 and Y3.

RESULTS: The obtained polynomial models had prediction R(2) values of 0.645, 0.947 and 0.795 for Y1, Y2 and Y3, respectively. Contour, Piepel's response trace, perturbation, and interaction plots were drawn for responses representation. The optimized formulation, A: 265 mg, B: 10 mg, C: 40 mg, D: zero g and E: 120 s, had desirability of 0.9526. The actual response values for the optimized formulation were within the two-sided 95% prediction intervals and were close to the predicted values with maximum percent deviation of 6.2%.

CONCLUSIONS: This indicates the validity of combined MPV design and modeling for optimization of transfersomal formulations as an example of nanovesicular systems.

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