Background:
Acne is the pilosebaceous units' disorder. The most important cause of acne is the colonization of bacteria in the follicles. Among antibiotics, doxycycline hyclate kills a wide range of bacteria.
Objectives:
To prevent oral administration's side effects, overcome the barriers of conventional topical treatment, and improve the therapeutic effectiveness, this drug was loaded into niosomal nanocarriers for topical application.
Methods:
Doxycycline hyclate was loaded into four niosomal formulations prepared by the thin-film hydration method with different percentages of constituents. Drug-containing niosomal systems were evaluated for morphological properties via scanning electron microscopy, particle size, drug entrapment efficiency, zeta potential, in vitro drug release, physical stability after 60 days, in vitro drug permeation through rat skin, in vitro drug deposition in rat skin, toxicity on human dermal fibroblasts (HDF) by MTT method after 72 hours, and antibacterial properties against the main acne-causing bacteria via antibiogram test.
Results:
The best formulation had the appropriate particle size of 362.88 ± 13.05 nm to target follicles, entrapment efficiency of 56.3 ± 2.1%, the zeta potential of - 24.46±1.39 mV, in vitro drug release of 54.93 ± 1.99% after 32 hours, and the lowest permeation of the drug through the rat skin among all other formulations. Improved cell viability, increased antibacterial activity, and an approximately three-fold increase in drug deposition were the optimal niosomal formulation features relative to the free drug.
Conclusion:
This study demonstrated the ability of nano-niosomes containing doxycycline hyclate to treat skin acne compared with the free drug.
Acne is the pilosebaceous units' disorder. The most important cause of acne is the colonization of bacteria in the follicles. Among antibiotics, doxycycline-hyclate kills a wide range of bacteria. To prevent oral administration's side effects, overcome the barriers of conventional topical treatment, and improve the therapeutic effectiveness, doxycycline-hyclate was loaded into four niosomal formulations with different percentages of constituents (span 60 and cholesterol) prepared by the thin-film hydration method. Then, one of the four formulations with the most appropriate particle size of 362.88 ± 13.05 nm to target the follicles, percentage of drug entrapment efficiency of 56.3 ± 2.1%, in vitro drug release of 54.93 ± 1.99% after 32 hours, and the lowest permeation of the drug through the Wistar rat skin, was selected. Then, its toxicity on human dermal fibroblasts (HDF) by MTT method after 72 hours, its antibacterial activity against the main acne-causing bacteria via antibiogram test, and its effect on Wistar rat skin drug deposition were measured. Improved cell viability, increased antibacterial activity, and an approximately three-fold increase in drug deposition were the optimal niosomal formulation features relative to the free drug. Overall, this study demonstrated the ability of nano-niosomes containing doxycycline-hyclate to treat skin acne.
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