Enhancement of the Mechanical and Drug-Releasing Properties of Poloxamer 407 Hydrogels with Casein

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 las...

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Bibliographic Details
Published in:	Pharmaceutical research Vol. 38; no. 3; pp. 515 - 522
Main Authors:	Tundisi, Louise Lacalendola, Yang, Rong, Borelli, Luiz Phellipe Pozzuto, Alves, Thais, Mehta, Manisha, Chaud, Marco Vinícius, Mazzola, Priscila Gava, Kohane, Daniel S.
Format:	Journal Article
Language:	English
Published:	New York Springer US 01-03-2021 Springer Springer Nature B.V
Subjects:	Adhesiveness Administration, Topical Analysis Animals Biochemistry Biomedical and Life Sciences Biomedical Engineering and Bioengineering Biomedicine Body temperature Bupivacaine Bupivacaine - administration & dosage Bupivacaine - chemistry Bupivacaine - pharmacokinetics Casein Caseins - chemistry Controlled release Drug Carriers - chemistry Drug Compounding Drug Liberation Excipients - chemistry Humans Hydrogels Hydrogels - chemistry Hydrophobicity Male Mechanical Phenomena Mechanical properties Medical Law Patient compliance Pharmacology/Toxicology Pharmacy Poloxamer - chemistry Rats Rats, Sprague-Dawley Research Paper Rheology Rhodamines - administration & dosage Rhodamines - chemistry Rhodamines - pharmacokinetics Skin Skin diseases Temperature Viscosity casein poloxamer 407 drug delivery mixed micelles topical treatment
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Summary:	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.
ISSN:	0724-8741 1573-904X
DOI:	10.1007/s11095-021-03017-9