title: Intravaginal Delivery of Polyphenon 60 and Curcumin Nanoemulsion Gel.
abstract: Polyphenon 60 (P60) and curcumin (CUR) were loaded in a single nanoemulsion system and their combined antibacterial action was studied against uropathogenic Escherichia coli. To enhance availability at target organs and to inhibit enzymatic degradation in gastro intestinal tract, vaginal route of administration was explored. P60 + CUR nanoemulsion (NE) was formulated by ultra-sonication and optimized using Box-Behnken design. Optimized NE showed Z-average of 211.2 nm, polydispersity index of 0.343, and zeta potential of -32.7 mV. Optimized P60+ CUR NE was characterized by stability testing and transmission electron microscopy, and it was observed that NE was stable at 4°C for 30 days and monodisperse in nature with particle size of 195-205 nm. P60+ CUR NE was further formulated as gel and characterized by viscosity, growth curve analysis, and in vitro permeation studies. In vitro drug permeation studies in simulated vaginal media showed maximum permeation (84 ± 0.21%) of curcumin within 5 h and (91 ± 0.16%) of P60 within 8 h. Both the drugs maintained sustained permeation for 12 h. To investigate the transport via intravaginal route, gamma scintigraphy and biodistribution study of P60 + CUR NBG was performed on Sprague-Dawley rats using99mtechnetium pertechnetate for radiolabeling to P60 molecule. Following intravaginal administration, P60 + CUR NBG dispersed in the kidney and urinary bladder with (3.07 ± 0.15) and (3.35 ± 0.45) percentage per gram after 3 h for P60 and CUR, respectively, and remained active for 12 h. Scintigraphy images suggested that the P60 + CUR NBG given by intravaginal route led to effective distribution of actives in urinary tract, and this observation was in agreement with the biodistribution results.
authors.affiliation: Department of Biotechnology, Jaypee Institute of Information Technology, A-10, Sector 62, Noida, UP, 201307, India.
authors.forename: Atinderpal
authors.initials: A
authors.lastname: Kaur
authors.affiliation: Department of Biotechnology, Jaypee Institute of Information Technology, A-10, Sector 62, Noida, UP, 201307, India.
authors.forename: Yashaswee
authors.initials: Y
authors.lastname: Saxena
authors.affiliation: Department of Biotechnology, Jaypee Institute of Information Technology, A-10, Sector 62, Noida, UP, 201307, India.
authors.forename: Rakhi
authors.initials: R
authors.lastname: Bansal
authors.affiliation: Department of Biotechnology, Jaypee Institute of Information Technology, A-10, Sector 62, Noida, UP, 201307, India.
authors.forename: Sonal
authors.initials: S
authors.lastname: Gupta
authors.affiliation: Division of CBRN Defence, Institute of Nuclear Medicine and Allied Sciences, Brig SK Mazumdar Marg, Delhi, 110054, India.
authors.forename: Amit
authors.initials: A
authors.lastname: Tyagi
authors.affiliation: Division of CBRN Defence, Institute of Nuclear Medicine and Allied Sciences, Brig SK Mazumdar Marg, Delhi, 110054, India.
authors.forename: Rakesh Kumar
authors.initials: RK
authors.lastname: Sharma
authors.affiliation: Faculty of Pharmacy, Jamia Hamdard, Hamdard Nagar, New Delhi, 110062, India.
authors.forename: Javed
authors.initials: J
authors.lastname: Ali
authors.affiliation: National Institute of Immunology, Aruna Asaf Marg, New Delhi, 110067, India.
authors.forename: Amulya Kumar
authors.initials: AK
authors.lastname: Panda
authors.affiliation: Department of Biotechnology, Jaypee Institute of Information Technology, A-10, Sector 62, Noida, UP, 201307, India.
authors.forename: Reema
authors.initials: R
authors.lastname: Gabrani
authors.affiliation: Department of Biotechnology, Jaypee Institute of Information Technology, A-10, Sector 62, Noida, UP, 201307, India. shweta.dang@jiit.ac.in.
authors.forename: Shweta
authors.initials: S
authors.lastname: Dang
mesh_terms: D000282:Administration, Intravaginal; D000818:Animals; D000890:Anti-Infective Agents / Q000008:administration & dosage / Q000493:pharmacokinetics; D003474:Curcumin / Q000008:administration & dosage / Q000493:pharmacokinetics; D004195:Disease Models, Animal; D004337:Drug Carriers; D004655:Emulsions; D004927:Escherichia coli Infections / Q000188:drug therapy; D008297:Male; D053758:Nanoparticles / Q000627:therapeutic use*; D010316:Particle Size; D010636:Phenols / Q000008:administration & dosage / Q000493:pharmacokinetics; D051381:Rats; D017207:Rats, Sprague-Dawley; D014018:Tissue Distribution; D016896:Treatment Outcome
chemical_list: D000890:Anti-Infective Agents; D004337:Drug Carriers; D004655:Emulsions; D010636:Phenols; C506663:polyphenon B; D003474:Curcumin
keywords: biodistribution; curcumin; intravaginal drug delivery; polyphenon 60; uropathogenic