Resveratrol-piperine loaded mixed micelles: formulation, characterization, bioavailability, safety and in vitro anticancer activity

RSC Advances ◽  
2016 ◽  
Vol 6 (114) ◽  
pp. 112795-112805 ◽  
Author(s):  
Prakash Jadhav ◽  
C. Bothiraja ◽  
Atmaram Pawar

Novel RES-carrying piperine loaded mixed micelles (RES-P-MM) composed of Poloxamer 407 and d-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) were developed to enhance the solubility, oral bioavailability and anticancer potency of RES.

2016 ◽  
Vol 18 (6) ◽  
pp. 2037-2044 ◽  
Author(s):  
Pramod Kumar ◽  
Rajendra Kumar ◽  
Bhupinder Singh ◽  
Ruchi Malik ◽  
Gajanand Sharma ◽  
...  

Nanomedicine ◽  
2021 ◽  
Vol 16 (5) ◽  
pp. 373-389
Author(s):  
Geetha Maniam ◽  
Chun-Wai Mai ◽  
Mohd Zulkefeli ◽  
Ju-Yen Fu

Aim: To synthesize niosomes co-encapsulating gemcitabine (GEM) and tocotrienols, and physicochemically characterize and evaluate the antipancreatic effects of the nanoformulation on Panc 10.05, SW 1990, AsPC-1 and BxPC-3 cells. Materials & methods: Niosomes-entrapping GEM and tocotrienols composed of Span 60, cholesterol and D-α-tocopheryl polyethylene glycol 1000 succinate were produced by Handjani-Vila and film hydration methods. Results: The film hydration produced vesicles measuring 161.9 ± 0.5 nm, approximately 50% smaller in size than Handjani-Vila method, with maximum entrapment efficiencies of 20.07 ± 0.22% for GEM and 34.52 ± 0.10% for tocotrienols. In Panc 10.05 cells, GEM’s antiproliferative effect was enhanced 2.78-fold in combination with tocotrienols. Niosomes produced a significant ninefold enhancement in cytotoxicity of the combination, supported by significantly higher cellular uptake of GEM in the cells. Conclusion: This study is a proof of concept on the synthesis of dual-drug niosomes and their efficacy on pancreatic cancer cells in vitro.


Pharmaceutics ◽  
2019 ◽  
Vol 11 (9) ◽  
pp. 476 ◽  
Author(s):  
Pescina ◽  
Lucca ◽  
Govoni ◽  
Padula ◽  
Favero ◽  
...  

This paper addresses the problem of ocular delivery of lipophilic drugs. The aim of the paper is the evaluation of polymeric micelles, prepared using TPGS (d-α-Tocopheryl polyethylene glycol 1000 succinate), a water-soluble derivative of Vitamin E and/or poloxamer 407, as a vehicle for the ocular delivery of dexamethasone, cyclosporine, and econazole nitrate. The research steps were: (1) characterize polymeric micelles by dynamic light scattering (DLS) and X-ray scattering; (2) evaluate the solubility increase of the three drugs; (3) measure the in vitro transport and conjunctiva retention, in comparison to conventional vehicles; (4) investigate the mechanisms of enhancement, by studying drug release from the micelles and transconjunctival permeation of TPGS; and (5) study the effect of micelles application on the histology of conjunctiva. The data obtained demonstrate the application potential of polymeric micelles in ocular delivery, due to their ability to increase the solubility of lipophilic drugs and enhance transport in and across the conjunctival epithelium. The best-performing formulation was the one made of TPGS alone (micelles size ≈ 12 nm), probably because of the higher mobility of these micelles, an enhanced interaction with the conjunctival epithelium, and, possibly, the penetration of intact micelles.


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