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Open AccessArticle

Preparation and Optimization of In Situ Gel Loaded with Rosuvastatin-Ellagic Acid Nanotransfersomes to Enhance the Anti-Proliferative Activity

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Department of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi Arabia
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Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Beni-Suef University, Beni-Suef 62511, Egypt
*
Author to whom correspondence should be addressed.
Pharmaceutics 2020, 12(3), 263; https://doi.org/10.3390/pharmaceutics12030263
Received: 10 February 2020 / Revised: 5 March 2020 / Accepted: 12 March 2020 / Published: 13 March 2020
(This article belongs to the Section Nanomedicine and Nanotechnology)
The objective of this study was to develop an optimized sustained-release nanotransfersomes (NTS) based in situ gel formulation of rosuvastatin (RO) combined with ellagic acid (EA) antioxidant, to enhance cytotoxic and anti-proliferative activity against tongue carcinoma. The concentrations of lecithin, Tween 80, and d-tocopherol polyethylene glycol succinate (TPGS) were considered as independent variables. Particle size, entrapment, and stability were selected as dependent variables. The obtained formulation containing 25% lecithin, 20% Tween 80, and TPGS 15% fulfilled the prerequisites of the optimum formulation. RO-NTS loaded in situ gel was prepared and optimized for concentrations of Poloxamer 407, and Carbopol, using statistical design. Drug release from in situ gel showed a sustained release profile. The RO IC50 was decreased by half for the in situ gel in comparison to plain RO and RO-EA-NTS. A significant amount of caspase-3 was detected in all the formulation treatments. The studies indicated that EA’s synergistic anti-oxidant effect owing to a high affinity to the PGP efflux transporter and higher penetration in the RO-NTS formulation led to a higher inhibition against human chondrosarcome-3 cancer cell lines. RO-EA NTS–loaded in situ gel had a sustained release that could be significant in localized therapy as an alternative to surgery in the treatment of aggressive tongue carcinoma. View Full-Text
Keywords: rosuvastatin; antioxidant; ellagic acid; box behnken design; nanotransferosomes; in situ gel; human chondrosarcome-3 cell line; tongue carcinoma rosuvastatin; antioxidant; ellagic acid; box behnken design; nanotransferosomes; in situ gel; human chondrosarcome-3 cell line; tongue carcinoma
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MDPI and ACS Style

Hosny, K.M.; Rizg, W.Y.; Khallaf, R.A. Preparation and Optimization of In Situ Gel Loaded with Rosuvastatin-Ellagic Acid Nanotransfersomes to Enhance the Anti-Proliferative Activity. Pharmaceutics 2020, 12, 263.

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