RESUMO
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.
RESUMO
Transdermal drug delivery systems (TDDS) for antibiotics have seen significant advances in recent years that aimed to improve the efficacy and safety of these drugs. TDDS offer many advantages over other conventional delivery systems such as non-invasiveness, controlled-release pattern, avoidance of first-pass metabolism. The objective of this review is to provide an overview on the recent advances in the TDDS of different groups of antibiotics including ß-lactams, tetracyclines, macrolides, and lincosamides, utilized for their effective delivery through the skin and to explore the challenges associated with this field. The majority of antibiotics do not have favorable properties for passive transdermal delivery. Thus, novel strategies have been employed to improve the delivery of antibiotics through the skin, such as the use of nanotechnology (nanoparticles, solid-lipid nanoparticles, nanoemulsions, vesicular carriers, and liposomes) or the physical enhancement techniques like microneedles and ultrasound. In conclusion, the transdermal delivery systems could be a promising method for delivering antibiotics that have the potential to improve patient outcomes and enhance the efficacy of drugs. Further research and development are still needed to explore the potential of delivering more antibiotic drugs by using various transdermal drug delivery approaches.