de Andrade Diego Fontana, Fontana Márcia Camponogara, Pohlmann Adriana Raffin, Guterres Silvia Stanisçuaski, Carlos Ruy, Beck Ruver
J Nanosci Nanotechnol. 2015 Jan;15(1):875-9. doi: 10.1166/jnn.2015.9183.
An immunosuppressive effect with drug release control and higher NTPDase activity in the treatment of contact dermatitis was previously reported for a hydrogel containing 0.05% clobetasol propionate-loaded lipid-core nanocapsules (HG-LNC-CP) compared to a hydrogel containing the non-encapsulated drug (HG-CP). In order to investigate the factors underlying this different performance, we evaluated the in vitro skin permeation/penetration of CP from both formulations (HG-LNC-CP and HG-CP). CP did not permeate to the receptor medium during the experiment (24 h), but penetrated into the stratum corneum and viable skin (epidermis and dermis) in significant amounts after 24 h, regardless the type of the formulation. Comparing both formulations, although the relative amount of CP in each skin layer was not affected by the nanoencapsulation, HG-LNC-CP was able to reduce in 5.8, 6.9 and 3.7 times the amount of CP released into the stratum corneum, epidermis and dermis respectively. In this way, the higher effect of HG-LNC-CP previously observed could be due to the controlled drug penetration rate into the skin layers. Moreover, HG-LNC-CP reduces the chances of the corticosteroid to be absorbed systemically as the amount of CP reaching the dermis was reduced. The study reinforces the HG-LNC-CP as a promising dermatological nanomedicine for the treatment of skin disorders.
先前有报道称，与含有未包封药物的水凝胶（HG-CP）相比，含有0.05%丙酸氯倍他索负载脂质核纳米胶囊的水凝胶（HG-LNC-CP）在治疗接触性皮炎时具有药物释放控制和更高的NTPDase活性的免疫抑制作用。为了研究这种不同性能背后的因素，我们评估了两种制剂（HG-LNC-CP和HG-CP）中CP的体外皮肤渗透/穿透情况。在实验期间（24小时），CP未渗透到受体介质中，但24小时后大量渗透到角质层和活皮肤（表皮和真皮）中，无论制剂类型如何。比较两种制剂，虽然纳米包封不影响各皮肤层中CP的相对量，但HG-LNC-CP能够分别将释放到角质层、表皮和真皮中的CP量减少5.8倍、6.9倍和3.7倍。这样，先前观察到的HG-LNC-CP的更高效果可能是由于药物向皮肤层的渗透速率得到控制。此外，由于到达真皮的CP量减少，HG-LNC-CP降低了皮质类固醇被全身吸收的可能性。该研究强化了HG-LNC-CP作为一种有前途的用于治疗皮肤疾病的皮肤纳米药物的地位。
