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Cerasomes (CS), evolved from liposomes, are novel drug-delivery systems that have potential medical application as carriers for drugs or active ingredients. Although many studies have been conducted on the pharmaceutical and physicochemical properties of CS, the role of CS in influencing the in vivo plasma and topical pharmacokinetics and efficacy of topical drug delivery remain unclear. In this context, we chose cryptotanshinone (CTS) as a model drug for the preparation of CTS-CS by means of the ethanol injection method to investigate their in vitro/in vivo drug-release behavior and in vivo efficacy. (1) In in vitro studies, CTS-CS gel was proven to be capable of achieving a higher permeation rate and significant accumulation in the dermis of isolated rat skin using Franz diffusion cells. (2) In in vivo studies, microdialysis experiments used to measure the plasma and topical pharmacokinetics demonstrated that the CS had a high drug concentration, short peak time, and slow elimination. Meanwhile, the plasma area under the concentration-time curve of CTS-CS gel was less than half that for the CTS gel in 12 h, which indicates that the drug bioavailability dramatically increased in the experiments. (3) In in vivo efficacy studies, we duplicated a rat acne model and performed antiacne efficacy experiments. The CTS-CS gel improved the antiacne efficacy compared to that of ordinary CTS gel. Moreover, it inhibited the expression of interleukin-1α and androgen receptors effectively. All of these results show that CTS-CS gel has significant potential for the treatment of acne induced by inflammation and excessive secretion of androgen, suggesting that CS formulations were designed as a good therapeutic option for skin disease.

Cryptotanshinone-Loaded Cerasomes Formulation: In Vitro Drug Release, in Vivo Pharmacokinetics, and in Vivo Efficacy for Topical Therapy of Acne