Journal article
Effect of Salt Form on Gelation and Drug Delivery Properties of Diclofenac-Loaded Poloxamer Gels for Delivery to Impaired Skin
Pharmaceutical research, Vol.39, pp.2515-2527
08/24/2022
DOI: 10.1007/s11095-022-03356-1
PMCID: PMC9578569
PMID: 36002613
Abstract
Purpose
Treating chronic wounds is a significant clinical challenge, and a topical product would be ideal for pain management. Poloxamer 407, a thermosensitive polymer, would allow an analgesic drug to be topically applied to a wound as a liquid that transitions to a gel at physiologic temperature. Using diclofenac as a model analgesic drug, our goal was to determine effects of salt form on poloxamer gelation and drug delivery from poloxamer gels applied to excised skin with impaired barrier function.
Methods
Gelation properties of 17% and 20% poloxamer gels loaded with 0.4 to 1.7% diclofenac sodium, potassium, epolamine, or diethylamine were evaluated rheologically. Drug release and delivery were quantified using cellulose membranes, porcine skin, and tape-stripped porcine skin.
Results
Poloxamer gelation temperature increased with higher diclofenac concentration, regardless of salt form; the magnitude of increase varied in the following order: sodium>potassium>diethylamine>epolamine. Gelation temperature differences resulting from the various counterions generally matched previously observed trends of ion-specific effects on macromolecule solubility (the Hofmeister series). Despite changes in gelation behavior, we observed minimal corresponding effects on drug release or delivery. There were no significant differences in diclofenac released or delivered through intact porcine skin over 48 h. However, in studies with impaired (tape-stripped) skin, diclofenac delivery was slowest overall with the epolamine salt.
Conclusion
Varying the salt form of a model analgesic drug can impact gelation and drug delivery characteristics of poloxamer systems. Further study of the mechanisms of these changes will be important for continued development of topical poloxamer products for clinical wound care.
Details
- Title: Subtitle
- Effect of Salt Form on Gelation and Drug Delivery Properties of Diclofenac-Loaded Poloxamer Gels for Delivery to Impaired Skin
- Creators
- Jackson Russo - University of IowaJennifer FiegelNicole K Brogden
- Resource Type
- Journal article
- Publication Details
- Pharmaceutical research, Vol.39, pp.2515-2527
- DOI
- 10.1007/s11095-022-03356-1
- PMID
- 36002613
- PMCID
- PMC9578569
- NLM abbreviation
- Pharm Res
- ISSN
- 0724-8741
- eISSN
- 1573-904X
- Grant note
- name: NIH, award: R35GM124551; name: NIH, and the Center for Biocatalysis and Bioprocessing, University of Iowa, award: T32GM008365
- Language
- English
- Date published
- 08/24/2022
- Academic Unit
- Dermatology; Pharmaceutical Sciences and Experimental Therapeutics; Chemical and Biochemical Engineering
- Record Identifier
- 9984297658302771
Metrics
106 Record Views