title: Perspectives of nanoemulsion assisted oral delivery of docetaxel for improved chemotherapy of cancer.
abstract: BACKGROUND
  Nanoemulsions (NE) are one of the robust delivery tools for drugs due to their higher stability and efficacy.
  
  
  OBJECTIVE
  The purpose of present investigation is to develop stable, effective and safe NE of docetaxel (DTX).
  
  
  METHODS
  Soybean oil, lecithin, Pluronic F68, PEG 4000 and ethanol were employed as excipients and NEs were prepared by hot homogenization followed by ultra-sonication. NEs were optimized and investigated for different in vitro and in vivo parameters viz. droplet size, poly dispersity index, charge; zeta potential, drug content and in vitro drug release, in vitro cytotoxicity, in vitro cell uptake and acute toxicity. Transmission electron microscopy was performed to study morphology and structure of NEs. Stability studies of the optimized formulation were performed.
  
  
  RESULTS
  Droplet size, poly dispersity index, zeta potential, drug content and in vitro drug release were found to be 233.23 ± 4.3 nm, 0.24 ± 0.010, -43.66 ± 1.9 mV, 96.76 ± 1.5%, 96.25 ± 2.1%, respectively. NE F11 exhibited higher cell uptake (2.83 times than control) and strong cytotoxic activity against MCF-7 cancer cells (IC50; 13.55 ± 0.21 µg/mL at 72 h) whereas no toxicity or necrosis was observed with liver and kidney tissues of mice at a dose of 20 mg/kg. Transmission electron microscopy ensured formation of poly-dispersed and spherical droplets in nanometer range. NE F11 (values indicated above) was selected as the optimized formulation based on the aforesaid parameters.
  
  
  CONCLUSIONS
  Conclusively, stable, effective and safe NE was developed which might be used as an alternative DTX therapy.
authors.affiliation: a Pharmaceutics Division , CSIR-Central Drug Research Institute , Lucknow , India and.|b Amity Institute of Pharmacy, Amity University , Lucknow , India.
authors.forename: Prerna
authors.initials: P
authors.lastname: Verma
authors.affiliation: a Pharmaceutics Division , CSIR-Central Drug Research Institute , Lucknow , India and.
authors.forename: Jaya Gopal
authors.initials: JG
authors.lastname: Meher
authors.affiliation: a Pharmaceutics Division , CSIR-Central Drug Research Institute , Lucknow , India and.
authors.forename: Shalini
authors.initials: S
authors.lastname: Asthana
authors.affiliation: a Pharmaceutics Division , CSIR-Central Drug Research Institute , Lucknow , India and.
authors.forename: Vivek K
authors.initials: VK
authors.lastname: Pawar
authors.affiliation: b Amity Institute of Pharmacy, Amity University , Lucknow , India.
authors.forename: Mohini
authors.initials: M
authors.lastname: Chaurasia
authors.affiliation: a Pharmaceutics Division , CSIR-Central Drug Research Institute , Lucknow , India and.
authors.forename: Manish K
authors.initials: MK
authors.lastname: Chourasia
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000737:chemistry / Q000378:metabolism / Q000633:toxicity; D001943:Breast Neoplasms / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D002470:Cell Survival; D000077143:Docetaxel; D004305:Dose-Response Relationship, Drug; D004337:Drug Carriers; D004339:Drug Compounding; D004355:Drug Stability; D004655:Emulsions; D000431:Ethanol / Q000737:chemistry; D005079:Excipients / Q000737:chemistry; D005260:Female; D006358:Hot Temperature; D006801:Humans; D020128:Inhibitory Concentration 50; D054709:Lecithins / Q000737:chemistry; D061986:MCF-7 Cells; D051379:Mice; D046529:Microscopy, Electron, Transmission; D053758:Nanoparticles; D036103:Nanotechnology; D010316:Particle Size; D020442:Poloxamer / Q000737:chemistry; D011092:Polyethylene Glycols / Q000737:chemistry; D012995:Solubility; D013024:Soybean Oil / Q000737:chemistry; D013499:Surface Properties; D013501:Surface-Active Agents / Q000737:chemistry; D043823:Taxoids / Q000008:administration & dosage* / Q000737:chemistry / Q000378:metabolism / Q000633:toxicity; D013678:Technology, Pharmaceutical / Q000379:methods; D014465:Ultrasonics
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D004655:Emulsions; D005079:Excipients; D054709:Lecithins; D013501:Surface-Active Agents; D043823:Taxoids; D020442:Poloxamer; D000077143:Docetaxel; D000431:Ethanol; D011092:Polyethylene Glycols; C000595214:polyethylene glycol 4000; D013024:Soybean Oil
keywords: Acute toxicity; MTT assay; droplet size; soybean oil; zeta potential