Topotecan-loaded lipid nanoparticles as a viable tool for the topical treatment of skin cancers.
J Pharm Pharmacol
; 69(10): 1318-1326, 2017 Oct.
Article
de En
| MEDLINE
| ID: mdl-28703281
ABSTRACT
OBJECTIVES:
This work aimed to evaluate semisolid formulations containing topotecan (TPT) loaded nanostructured lipid carriers (NLC) for topical treatment of skin cancers, as TPT is effective against a variety of tumours. A formulation which increases TPT skin permeation would be extremely desirable.METHODS:
TPT-NLC were prepared and incorporated in hydrogels with hydroxyethyl cellulose and chitosan (TPT-NLC-HEC and TPT-NLC-Ch, respectively). Control formulations were obtained by dispersing TPT in HEC and Ch hydrogels (TPT-HEC and TPT-Ch). KEYFINDINGS:
TPT-NLC-HEC and TPT-NLC-Ch showed to maintain the drug and nanoparticle dispersions stable for up to 30 days. When nanoparticles were incorporated into gels, TPT release was significantly decreased (P < 0.05). Still, TPT-NLC-HEC increased 2.37 times permeation compared with TPT-HEC (11.9 and 5.0 µg/cm2 , respectively). Cell culture experiments with B16F10 melanoma demonstrated that nanoencapsulation significantly increased TPT cytotoxicity (P < 0.05). TPT-NLC was more toxic than free TPT, with IC50 value of 5.74 µg/ml, whereas free TPT had an IC50 > 20 µg/ml. As skin permeated values of TPT from developed formulation (TPT-NLC) were superior to melanoma IC50, it can be extrapolated that chemotherapeutic permeated amounts may be sufficient for a therapeutic effect.CONCLUSIONS:
TPT-NLC-HEC may be a valuable tool for the topical treatment of skin cancers.Mots clés
Texte intégral:
1
Collection:
01-internacional
Base de données:
MEDLINE
Sujet principal:
Absorption cutanée
/
Tumeurs cutanées
/
Mélanome expérimental
/
Vecteurs de médicaments
/
Topotécane
/
Nanoparticules
Limites:
Animals
Langue:
En
Journal:
J Pharm Pharmacol
Année:
2017
Type de document:
Article
Pays d'affiliation:
Brésil