Abstract
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.
Highlights
Tongue cancer is a well-known type of mouth cancer
From the Box–Behnken factorial design, a total of 17 runs were projected by the design expert for three factors: egg lecithin (%) (X1); Tween 80 (%) (X2); and tocopherol polyethylene glycol succinate (TPGS) (%) (X3), which were varied at three different levels
Based on the desirability approach, a formulation containing Poloxamer 407-7% and Carbopol 934P-0.2% could fulfill the prerequisites of optimum formulation for preparing an RO-ellagic acid (EA) NTS loaded in situ gel
Summary
It develops as a result of uncontrolled cell divisions, which, in this case, are the squamous cells present on the tongue surface [1]. Statins are one of the most commonly prescribed drugs all over the world. They are well known for their cholesterol-lowering effect; they are mainly used to treat and protect against cardiovascular diseases [3]. Lovastatin increased the anticancer activity of doxorubicin against colon and breast cancer in mice [4,5]. Administration of statins combined with antioxidant compounds of natural origin can yield better results as shown in the combination of simvastatin and alpha-lipoic acid that improved toxicity against breast carcinoma cell lines [8]
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