RESUMO
OBJECTIVE: To compare the intradermal delivery effects of composite phospholipid liposomes composed of different proportions of soy phospholipids (SPC) and hydrogenated soy phospholipids (HSPC) on the fluorescent modified hydroxypropyl-β-cyclodextrin(HP-β-CD), and to optimize the phospholipid composition with the best skin retention. METHODS: The fluorescent probe, fluorescein isothiocyanate (FITC), was combined with HP-β-CD to prepare fluorescent modified cyclodextrin FITC-HP-β-CD. FITC-HP-β-CD was encapsulated in different composite phospholipid liposomes. The amount of the permeation in the receiving solution and skin retention of the cyclodextrin after 10 h were determined in the in vitro intradermal delivery experiment. RESULTS: The order of cyclodextrin permeation of liposomes in the receiving solution was SPC > S/H (3:1) > S/H (1:1) > S/H (1:3) > HSPC >FITC-HP-β-CD, while the order of cyclodextrin intradermal retention was S/H (1:1) > S/H (1:3) > HSPC > S/H (3:1) > SPC > FITC-HP-β-CD. CONCLUSION: Using SPC to prepare liposomes is more beneficial to promote the permeation of FITC-HP-β-CD into the skin than HSPC, but the addition of HSPC can increase the skin retention of FITC-HP-β-CD. The S/H(1:1) liposomes have the better intradermal delivery effect on the fluorescent modified cyclodextrin, of which the skin retention effect is the best.
RESUMO
To compare the penetration-enhancing effect of cinnamon oil and its main components (cinnamaldehyde) on ibuprofen and their self-percutaneous absorption behavior in vitro. Firstly, cinnamon oil was extracted by steam distillation, then the compositions were analyzed by gas chromatography mass spectrometry (GC-MS) and the cinnamaldehyde content in cinnamon oil was determined by high performance liquid chromatography (HPLC). With azone as positive control, ibuprofen as model drug, cinnamon oil and cinnamaldehyde as penetration enhancers (PE) were prepared and administered to the SD rat's abdominal skin. The penetration-enhancing effects of cinnamon oil and cinnamaldehyde and their own transdermal absorption properties were compared. The results showed that yield of cinnamon oil was (3.55±0.36)% (=3), and the cinnamaldehyde content in cinnamon oil was (73.48±0.21)% (=3). As compared with blank group, the enhancing rate (ER) of cinnamon oil, cinnamaldehyde, and azone was 3.56, 1.13, 2.47 respectively. The cumulative penetration rate of cinnamaldehyde in cinnamon oil and cinnamaldehyde monomer in 24 h was (63.30±0.98)%, (51.03±3.34)% (=4) respectively. The penetration-enhancing effect of cinnamon oil was significantly better than that of cinnamaldehyde, indicating the existence of muti-component synergy. The penetration rate of cinnamaldehyde in cinnamon oil was higher than that of cinnamaldehyde monomer, suggesting that a "pull effect" may be present.