retention of poloxamer-basedhydrogels for vaginal application in mouse and rat models.
10.1016/j.apsb.2017.03.003
- Author:
Yu LIU
1
;
Fujin YANG
1
;
Linglin FENG
2
;
Long YANG
1
;
Lingyun CHEN
3
;
Gang WEI
1
;
Weiyue LU
1
Author Information
1. Key Laboratory of Smart Drug Delivery, Ministry of Education, Fudan University, Shanghai 201203, China.
2. Shanghai Institute of Planned Parenthood Research, National Population and Family Planning Key Laboratory of Contraceptives Drugs and Devices, Shanghai 200032, China.
3. Yunnan University of Traditional Chinese Medicine, Kunming 650500, China.
- Publication Type:Journal Article
- Keywords:
AUC, area under curve;
EO, hydrophilic ethylene oxide;
F127, Poloxamer 407;
F68, poloxamer 188;
GEL1, 1% poloxamer 188 + 18% poloxamer 407;
GEL2, 6% poloxamer 188 + 18% poloxamer 407;
HLB, hydrophile--lipophile balance;
ICR, Institute of Cancer Research;
MRT, mean residence time;
MW, molecular weight;
N-9, Nonoxynol-9;
Nonoxinol-9;
PEO-PPO-PEO, poly(ethylene oxide)a-poly(propylene oxide)b-poly(ethylene oxide)a;
PO, hydrophobic propylene oxide;
Poloxamer;
RP-HPLC, reverse-phase high performance liquid chromatography;
Retention;
SVF, simulated vaginal fluid;
Thermosensitive hydrogel;
Vaginal administration
- From:
Acta Pharmaceutica Sinica B
2017;7(4):502-509
- CountryChina
- Language:English
-
Abstract:
The purpose of this study is to evaluate theretention capabilities of poloxamer-basedhydrogels for vaginal application with nonoxinol-9 as the model drug. Twohydrogel formulations, which contained 18% poloxamer 407 plus 1% poloxamer 188 (GEL1, relative hydrophobic) or 6% poloxamer 188 (GEL2, relative hydrophilic), were compared with respect to the rheological properties,hydrogel erosion and drug release. The vaginal retention capabilities of these hydrogel formulations were further determined in two small animal models, including drug quantitation of vaginal rinsing fluid in mice and isotope tracing withTc in rats. The two formulations exhibited similar phase transition temperatures ranging from 27 to 32 °C. Increasing the content of poloxamer 188 resulted in higher rheological moduli under body temperature, but slightly accelerated hydrogel erosion and drug release. When compared, GEL1 was eliminated significantly slower in rat vagina than GEL2, while the vaginal retention of these two hydrogel formulations behaved similarly in mice. In conclusion, increases in the hydrophilic content of formulations led to faster hydrogel erosion, drug release and intravaginal elimination. Rats appear to be a better animal model than mice to evaluate thehydrogel for vaginal application.
