Enhancement of the Mechanical and Drug-Releasing Properties of Poloxamer 407 Hydrogels with Casein
- 26 February 2021
- journal article
- research article
- Published by Springer Science and Business Media LLC in Pharmaceutical Research
- Vol. 38 (3), 515-522
- https://doi.org/10.1007/s11095-021-03017-9
Abstract
Purpose Topical therapy of local disease (e.g. skin) is advantageous over oral therapy since there is less systemic drug distribution (so fewer side-effects), no first-pass effect, etc. However, patient compliance with topical therapy can be poor as it may require many applications a day and can last months. Here we propose a topical controlled release formulation with thermoresponsive gelation at body temperature and improved adhesiveness, making it easier to remain in contact with the body. Methods The formulation contains two excipients, poloxamer 407 (P407) and casein. Casein can modify the properties of the hydrogel through molecular entanglement. In addition, tissue reaction and drug release profile were evaluated. Results Changes in casein concentration affected adhesive strength, viscosity, mechanical properties and drug release, presumably by hydrophobic interactions between casein and P407. Two different concentrations of P407 were tested with two different concentrations of casein. Formulations containing 5% and 10% casein released 80% of model drug in 48 h, while formulations without casein released the same fraction in around 24 h hours. Formulations with 10% casein had almost twice the adhesive strength of those without casein. Conclusions Addition of casein modified the mechanical properties and drug release rate of the hydrogel. There was no inflammation or injury after brief exposure in vivo.Keywords
Funding Information
- FAPESP (2017/10728-2, 2018/05421-8, 2018/07707-6)
- Foundation for the National Institutes of Health (R35 GM131728)
- Conselho Nacional de Desenvolvimento Científico e Tecnológico (301436/2017-7)
This publication has 27 references indexed in Scilit:
- Improved texture analysis for hydrogel characterization: Gel cohesiveness, adhesiveness, and hardnessJournal of Applied Polymer Science, 2011
- Mixed micellization between natural and synthetic block copolymers: β-casein and Lutrol F-127Physical Chemistry Chemical Physics, 2010
- Milk proteins as vehicles for bioactivesCurrent Opinion in Colloid & Interface Science, 2010
- Self-Assembly of Bovine β-Casein below the Isoelectric pHJournal of Agricultural and Food Chemistry, 2008
- Development and characterization of film forming polymeric solutions for skin drug deliveryEuropean Journal of Pharmaceutics and Biopharmaceutics, 2007
- β-Casein and Symmetrical Triblock Copolymer (PEO−PPO−PEO and PPO−PEO−PPO) Surface Properties at the Air−Water InterfaceLangmuir, 2004
- Rheological behavior of poloxamer 407 aqueous solutions during sol-gel and dehydration processesInternational Journal of Pharmaceutics, 1994
- Pluronic F-127 gels as a vehicle for topical administration of anticancer agents.CHEMICAL & PHARMACEUTICAL BULLETIN, 1984
- In vitro release of lidocaine from pluronic F-127 gelsInternational Journal of Pharmaceutics, 1981
- Artificial skin I. Preparation and properties of pluronic F‐127 gels for treatment of burnsJournal of Biomedical Materials Research, 1972