Physicochemical properties of pH-sensitive hydrogels based on hydroxyethyl cellulose–hyaluronic acid and for applications as transdermal delivery systems for skin lesions

• Published in: European journal of pharmaceutics and biopharmaceutics 2015-05, Vol.92, p.146-154
• Main Authors: Kwon, Soon Sik, Kong, Bong Ju, Park, Soo Nam
• Format: Article
• Language: English
• Subjects: Administration, Cutaneous; Animals; Anti-Bacterial Agents - administration & dosage; Anti-Bacterial Agents - pharmacokinetics; Anti-Bacterial Agents - pharmacology; Antimicrobial activity; Cellulose - analogs & derivatives; Cellulose - chemistry; Chalcones - administration & dosage; Chalcones - pharmacokinetics; Chalcones - pharmacology; Cross-Linking Reagents - chemistry; Drug Delivery Systems; Drug Liberation; Female; Hyaluronic acid; Hyaluronic Acid - chemistry; Hydrogel; Hydrogels; Hydrogen-Ion Concentration; Isoliquiritigenin; Microscopy, Electron, Scanning; pH-sensitive; Propionibacterium acnes; Propionibacterium acnes - drug effects; Rats; Rheology; Skin - metabolism; Skin - pathology; Skin Absorption; Smart hydrogel; Transdermal delivery system
• ISSN: 0939-6411; 1873-3441
• DOI: 10.1016/j.ejpb.2015.02.025

[Display omitted] •Hydrogels composed of HEC and HA were developed.•Physicochemical properties of the hydrogel were determined by analysis equipment.•The hydrogel containing isoliquiritigenin effectively inhibited the growth of acne.•The HECHA hydrogels may have a potential applicability as a transdermal delivery system. We investigated the physicochemical properties of pH-sensitive hydroxyethyl cellulose (HEC)/hyaluronic acid (HA) complex hydrogels containing isoliquiritigenin (ILTG), and discussed potential applications as transdermal delivery systems for the treatment of skin lesions caused by pH imbalance. HA has skin compatibility and pH functional groups and HEC serves as scaffold to build hydrogels with varied HCE:HA mass ratio. Hydrogels were synthesized via chemical cross-linking, and three-dimensional network structures were characterized via scanning electron microscopy (SEM). The swelling properties and polymer ratios of the hydrogels were investigated at pH values in the range 1–13. HECHA13 (i.e., an HEC:HA mass ratio of 1:3) was found to have optimal rheological and adhesive properties, and was used to investigate the drug release efficiency as a function of pH; the efficiency was greater than 70% at pH 7. Antimicrobial activity assays against Propionibacterium acnes were conducted to take advantage of the pH-sensitive properties of HECHA13. At pH 7, we found that HECHA13, which contained ILTG, inhibited the growth of P. acnes. Furthermore, HECHA13 was found to exhibit excellent permeability into the skin, which penetrated mostly via the hair follicle. These results indicate that this pH-sensitive hydrogel is effective as a transdermal delivery system for antimicrobial therapeutics, with potential applications in the treatment of acne.