不同分子量土鳖虫活性小肽凝胶的透皮特性研究

The study of the skin penetration characteristics with different molecular weight peptide gel woodlouse

关键词:  土鳖虫活性小肽  透皮吸收  凝胶剂

Key words:  Euplotes insecticidal small peptides  transdermal absorption  gels

摘要:

[目的] 研究不同分子量土鳖虫活性小肽凝胶的透皮特性，筛选土鳖虫活性小肽凝胶最佳组分。[方法] 采用酶解法和超滤法得到不同分子量段土鳖虫活性小肽（P1：M < 1KDa，P2：1KDa < M < 3KDa，P3：M > 3KDa），并采用folin法对3种组分进行含量测定。以肽含量为指标采用改良Franz扩散池法对比3种土鳖虫活性小肽凝胶剂与水溶液的透皮吸收率，并对最佳土鳖虫活性小肽凝胶组分筛选不同部位鼠皮透皮率，不同促渗剂及浓度的促渗效果。[结果] 不同分子量土鳖虫活性小肽的肽含量顺序为P2（70.84%） > P3（52.08%） > P1（40.13%），3种土鳖虫活性小肽凝胶剂透皮吸收率分别为P1：96.16%、P2：81.92%、P3：62.45%，水溶液组分的透皮吸收率为P1：62.92%、P2：52.28%、P3：38.26%，P1凝胶剂的透皮吸收率最佳。P1凝胶剂组分腹部皮肤透皮率为96.19%，大于背部皮肤透皮率54.03%。3种促渗剂对P1凝胶组分的促渗作用为氮酮 > PEG400 > 油酸，氮酮的促渗效果优于其他促渗剂。不同浓度氮酮促渗剂促渗效果差异不大，1%浓度即可满足实验要求。[结论] 土鳖虫3种活性小肽组分中，P1凝胶透皮渗透率更高，优选的P1凝胶组成合理。

Abstract:

[Objective] To study the transdermal properties of small peptides with different molecular weight, screening the best components of active peptide gel of eupolyphaga.[Methods] Enzymatic hydrolysis and ultrafiltration were used to obtain small peptides with different molecular weigh(P1:M < 1KDa,P2:1KDa < M < 3KDa, P3:M > 3KDa), and the content of the three components was determined by folin method. The transdermal absorption rate of three small turtle insecticidal active peptidoglycans and aqueous solution was compared with the modified Franz diffusion pool method with the peptide content as the index,and the skin permeation rate of different parts was screened for the best peptidoglycan active gelatin component, the effect of different penetration enhancers and concentration.[Results] The content of peptides in small peptides with different molecular weights was P2 (70.84%) > P3 (52.08%) > P1 (40.13%), the transdermal absorption rates of the three small turtle insects were P1:96.16%、P2:81.92%、P3:62.45%,the transdermal absorption rate of the aqueous solution component is P1:62.92%、P2:52.28%、P3:38.26%,P1 gels have the best transdermal absorbance.P1 gellant component abdominal skin transdermal rate was 96.19%,greater than the back skin transdermal rate of 54.03%.The effect of three kinds of penetration enhancers on the gelation of P1 gel was Azone > PEG400 > oleic acid,the effect of nitroprusside is better than that of other penetration enhancers. There was no significant difference in the effect of different concentration of nitrilacin enhancer,1% concentration to meet the experimental requirements.[Conclusions] Among the three active small peptide components of Eupolyphaga sinensis, the transdermal permeability of P1 gel was higher, and the preferred P1 gel composition was reasonable.