Transdermal Delivery System of Doxycycline-Loaded Niosomal Gels: Toward Enhancing Doxycycline Stability.

Abstract

Doxycycline (DOX) is an antimicrobial agent that is susceptible to photosensitivity and thermal degradation. It addition, it causes gastrointestinal side effects when taken orally. Therefore, the development of alternative formulations is necessary to improve drug stability and promote patient compliance. The aim of the present study was to encapsulate DOX in niosomes as a nanocarrier to deliver DOX transdermally and enhance its stability in the formulation. DOX niosomes were prepared using nonionic surfactants, cholesterol, and dihexadecyl phosphate (DCP). After that, niosomes were characterized in terms of practical size (PS), zeta potential (ZP), morphology, and entrapment efficacy (EE%). DOX niosomal gels were then prepared using Carbopol and penetration enhancers (poly(ethylene glycol) 400 (PEG 400) and propylene glycol (PG)). The flux of DOX from the optimized formula was 322.86 μg/cm2/h over 5 h, which equates to 71.2% of DOX. Furthermore, neither the DOX niosomal gel (D3) nor the comparable blank niosomal gel had a negative influence on human dermal fibroblast (HDF) cells. The findings of the antimicrobial effectiveness of DOX niosomes indicated that the niosomal formulation improved the antibacterial activity of DOX against E. coli. Permeation studies demonstrated significantly higher DOX permeation when the niosomal gel was applied to rat skin, compared to the conventional gel. Permeability parameters such as flux and the permeability coefficient increased more than 10-fold using the niosomal gels compared with those of conventional gels. In conclusion, a new niosomal gel formulation could serve as an effective alternative for the commercially available form of DOX.