Amino-functionalized poloxamer 407 with both mucoadhesive and thermosensitive properties: preparation, characterization and application in a vaginal drug delivery system

Abstract

Lack of mucoadhesive properties is the major drawback to poloxamer 407 (F127)-based in situ hydrogels for mucosal administration. The objective of the present study was to construct a novel mucoadhesive and thermosensitive in situ hydrogel drug delivery system based on an amino-functionalized poloxamer for vaginal administration. First, amino-functionalized poloxamer 407 (F127-NH2) was synthesized and characterized with respect to its micellization behavior and interaction with mucin. Then using acetate gossypol (AG) as model drug, AG-loaded F127-NH2-based in situ hydrogels (NFGs) were evaluated with respect to rheology, drug release, ex vivo vaginal mucosal adhesion, in vivo intravaginal retention and local irritation after vaginal administration to healthy female mice. The results show that F127-NH2 is capable of forming a thermosensitive in situ hydrogel with sustained drug release properties. An interaction between positively charged F127-NH2 and negatively charged mucin was revealed by changes in the particle size and zeta potential of mucin particles as well as an increase in the complex modulus of NFG caused by mucin. Ex vivo and in vivo fluorescence imaging and quantitative analysis of the amount of AG remaining in mouse vaginal lavage all demonstrated greater intravaginal retention of NFG than that of an unmodified F127-based in situ hydrogel. In conclusion, amino group functionalization confers valuable mucoadhesive properties on poloxamer 407.

Therapeutics and delivery vehicles for local treatment of osteomyelitis

“…71,106 The list of these materials is extensive, as various combinations and novel formulations are often explored. 94,107,108 The release profiles of drugs from hydrogels vary depending on the nature of the interaction of drug with polymer, but there is typically an initial burst of therapeutic, which may be followed by a slow, low dose elution of residual therapeutic. 101,109 Hydrogels are generally biodegradable and may be cleared by the body in as early as 2 to 6 weeks.…”

Evaluation of double network hydrogel of poloxamer-heparin/gellan gum for bone marrow stem cells delivery carrier

“…Herein, a double network hydrogel (DNH) of GG hydrogel and synthetic hydrogel was developed to enhance biomechanical and physicochemical properties [25,28]. Poloxamer is an FDA approved hydrogel which is composed of hydrophobic poly (propylene oxide) (PPO) and hydrophilic poly (ethylene oxide) (PEO) [29][30][31]. Poloxamer hydrogel is proved to be effective in cell viability, non-toxicity, and biocompatibility.…”

Curcumin solid dispersion-loaded in situ hydrogels for local treatment of injured vaginal bacterial infection and improvement of vaginal wound healing

“…Therefore, CSDGs have good temperature sensitivity for intravaginal administration with a long‐term maintenance in the vagina. A similar in situ hydrogel to our formulation also showed the long‐term intravaginal retention effect …”