Browsing by Author "Sweed, Nabila M"

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Integrating Artifcial Intelligence with Quality by Design in the Formulation of Lecithin/Chitosan Nanoparticles of a Poorly Water‑Soluble Drug
(Springer International Publishing AG, 2023-08) Dawoud, Marwa H. S; Mannaa, Islam S; Abdel‑Daim, Amira ; Sweed, Nabila M
The aim of the current study is to explore the potential of artifcial intelligence (AI) when integrated with Quality by Design (QbD) approach in the formulation of a poorly water-soluble drug, for its potential use in carcinoma. Silymarin is used as a model drug for its potential efectiveness in liver cancer. A detailed QbD approach was applied. The efect of the critical process parameters was studied on each of the particle size, size distribution, and entrapment efciency. Response surface designs were applied in the screening and optimization of lecithin/chitosan nanoparticles, to obtain an optimized formula. The release rate was tested, where artifcial neural network models were used to predict the % release of the drug from the optimized formula at diferent time intervals. The optimized formula was tested for its cytotoxicity. A design space was established, with an optimized formula having a molar ratio of 18.33:1 lecithin:chitosan and 38.35 mg silymarin. This resulted in nanoparticles with a size of 161 nm, a polydispersity index of 0.2, and an entrapment efciency of 97%. The optimized formula showed a zeta potential of +38 mV, with well-developed spherical particles. AI successfully showed high predic- tion ability of the drug’s release rate. The optimized formula showed an enhancement in the cytotoxic efect of silymarin with a decreased IC50 compared to standard silymarin. Lecithin/chitosan nanoparticles were successfully formulated, with deep process and product understanding. Several tools were used as AI which could shift pharmaceutical formulations from experience-dependent studies to data-driven methodologies in the future.
A Quality by Design Paradigm for Albumin‑Based Nanoparticles: Formulation Optimization and Enhancement of the Antitumor Activity
(Springer New York, 2023-05) Dawoud, Marwa H. S; Abdel‑Daim, Amira ; Nour, Mai S; Sweed, Nabila M
Albumin nanoparticles are promising carriers for therapeutic agents, owing to their biocompatibility, safety, and versatility in fabrication. The formulation of albumin nanoparticles is highly afected by many product and process variables, resulting in a great variation in these nanoparticles. The aim of this work was to formulate and optimize albumin nanopar- ticles loaded with silymarin, as a model drug with low bioavailability, for the treatment of hepatocellular carcinoma, using quality by design (QbD) approach. Methods A thorough risk assessment for albumin nanoparticles formulation was developed and a complete quality product profle was defned using the QbD approach. A D-optimal design was used to optimize the amount of albumin and drug, which signifcantly afected the particle size (PS) and the entrapment efciency (EE%), which was further tested on hepa- tocellular carcinoma. Results A design space was constructed, with an optimized formula showing a PS of 135 nm, a polydispersity index (PDI) of 0.09, an EE% of 88%, and a zeta potential of−12.5 mV. The optimized formula (O1) with spherical particles, showed an extended-release rate as compared to free silymarin. Moreover, a pronounced anti-proliferation activity of O1 was observed on human hepatocellular carcinoma cell line HepG2 than the free drug. The fow cytometric analysis of the cell cycle showed a signifcant suppression of the S-phase after treating the HepG2 cell with O1, but not with free silymarin. Conclusion Thus, a detailed QbD study has been conducted, with deep product and process understanding, and resulted in a successful formulation of silymarin albumin nanoparticles for the suppression of hepatocellular carcinoma.
Response surface optimization of a cardioprotective compound through pharmacosomal drug delivery system: in vivo bioavailability and cardioprotective activity potential
(Springer Publishing Company, 2023-04) Dawoud, Marwa H. S; Zaafan, Mai A; Saleh, Sarah S; Mannaa, Islam M; Sweed, Nabila M
Vanillic acid (VA) is a phenolic compound with potential antioxidant activity, which improves ischemia-induced myocardial degeneration, by reducing oxidative stress; however, it sufers poor bioavailability owing to its poor solubility. VA-loaded pharmacosomes were optimized using a central composite design, where the efect of phosphatidylcholine:VA molar ratio and the precursor concentration were studied. An optimized formulation (O1) was prepared and tested for the release rate of VA, in vivo bioavailability, and cardioprotective potential on myocardial infarction-induced rats. The optimized formulation showed a particle size of 229.7 nm, polydispersity index of 0.29, and zeta potential of−30 mV. O1 showed a sustained drug release for 48 h. The HPLC–UV method was developed for the determination of VA in plasma samples using protein pre- cipitation. The optimized formulation showed a great improvement in the bioavailability as compared to VA. The residence time of the optimized formula was 3 times longer than VA. The optimized formulation showed a more potent cardioprotec- tive efect as compared to VA, via inhibition of the MAPK pathway with subsequent inhibition of PI3k/NF-κB signaling, in addition to its antioxidant efect. The optimized formulation showed normalization of many oxidative stress and infamma- tory biomarkers. Thus, a VA-loaded pharmacosome formulation with promising bioavailability and cardioprotective activity potential was prepared.