ABSTRACT
OBJECTIVE Hypericin, a powerful naturally photosensitizer in photodynamic therapy (PDT), is suitable for treating skin diseases involving excess capillary proliferation. In the present study, we aimed to evaluate the skin penetrability of a topically applied hypericin, expecting reducing the risk of prolonged skin photosensitivity, which often occurs after systemic administration. METHODS The Franz diffusion cell assay was performed to evaluate different penetration enhancers. In vivo studies, fluorescence microscopy was performed to examine the distribution of hypericin in the skin, macroscopic and microscopic analyses were also carried out to detect pathological changes in the skin after topical hypericin-PDT treatment. Immunohistochemistry was used to determine the expression of PECAM-1 in the treated skin. RESULTS 5% menthol facilitated hypericin penetrate the skin of nude mice most. The results of in vivo assays revealed that hypericin penetrated nude mice skin, spread to the dermis, and resulted in obvious photosensitivity reaction on the dermal capillaries. Moreover, skin injured by the photosensitive reaction induced by hypericin was replaced by normal skin 7 d after hypericin-PDT treat?ment. CONCLUSION Topical hypericin could penetrate nude mouse skin well and be great potential in PDT treatment of skin diseases.
ABSTRACT
Objective To prepare nasal triptolide nano liposome thermosensitive gel (TP-NLS-TG) and investigate the in vitro penetrability through nasal mucosa. Methods The triptolide nanoliposomes were prepared by high pressure homogenization method, and the ratio of poloxamer 407 (P-407) and poloxamer 188 (P-188) was selected, using the azone dosage and stirring time as investigation factors. Gelation temperature (GT) and homogeneity of TG (RSD) were used as evaluation indexes, and TP-NLS-TG was prepared by optimized prescription. An isolated mucosal permeability model was established by frog abdominal skin to carry out the in vitro permeation test of TP-NLS-TG in nasal mucosa. Results The best prescription was 12% P-407, 10% P-188, and 3% azone, and swelling time was 4 h. The TP-SLN gelation temperature of the gel was 32 ℃, and the RSD was 0.005%. In the first 8 h, the cumulative infiltration volume per unit area was (9.296 3 ± 0.614 7) μg/cm2, and the release curve in line with the Higuchi mathematical model. Conclusion The triptolide nano liposome gel prepared by the optimum technology has an accurate gelling temperature, and uniform content, which has good permeability, can be absorbed through the frog skin.
ABSTRACT
Objective To probe the methods of experimental research for the drug activities of the rat prostates. Methods With androgen and Staphylococcus aureus injected into the prostates, the bacterial prostatitis (BP) models and benign prostatic hyperplasia with bacterial prostatitis (BHP-BP) models were developed. The animals were fed with tetracycline and then the drug activities in the serum and the prostatic tissues, the quantities of the bacteria and the histopathlogical changes in the prostateic tissues were separately detected in different time. ResultsAfter ten days, the histopathlogical changes of the benign hyperplasia and mesenchyma were found in the prostatic tissue from BHP animals and acute suppurative inflammation were dicegnosed in prostatic tissue from the BP group after infected for two days. The drug activities of 22.44 mg/g in BP group and 20.26 mg/g in BPH-BP group were found until 3.5～4 hours and the values were higher than MBC of the tetracycline and the antibacterial activity of the sera at the same time. After 8 to 11 days of treating, the bacteria would not be isolated from the prostates of the animals with BP or BHP-BP. Stopping treatment a week 11 days after treating acute or chronic inflammation histopathlogical change did not be found in the prostates of animals with BP. 30 CFU of bacteria could be found in per gram tissue of prostate and both of the acute and chronic suppurative inflammation could be found in the BP group without treatment at the 28 days afterinfected.Conclusion The tetracycline activities in the prostates of rats with BP or BPH-BPis same as or even higher than that of serum and the MBC of the drug. The quantity of sensitive bacteria in prostates will be diminished and disappeared during treatment.