Nanodesign of new self-assembling core-shell gellan-transfersomes loading baicalin and in vivo evaluation of repair response in skin

• Published in: Nanomedicine Vol. 14; no. 2; pp. 569 - 579
• Main Authors: Manconi, Maria, Manca, Maria Letizia, Caddeo, Carla, Valenti, Donatella, Cencetti, Claudia, Diez-Sales, Octavio, Nacher, Amparo, Mir-Palomo, Silvia, Terencio, Maria Carmen, Demurtas, Davide, Gomez-Fernandez, Juan Carmelo, Aranda, Francisco José, Fadda, Anna Maria, Matricardi, Pietro
• Format: Journal Article
• Language: English
• Published: United States Elsevier Inc 01.02.2018
• Subjects: Administration, Cutaneous; Animals; Animals, Newborn; Anti-Inflammatory Agents, Non-Steroidal - administration & dosage; Anti-Inflammatory Agents, Non-Steroidal - chemistry; Drug Delivery Systems; Female; Flavonoids - administration & dosage; Flavonoids - chemistry; Gellan; In vivo studies; Inflammation - drug therapy; Liposomes - chemistry; Mice; Nanoparticles - chemistry; Polysaccharides, Bacterial - chemistry; Rheological studies; SAXS analysis; Skin - drug effects; Skin - injuries; Skin Absorption; Skin delivery; Swine; Transfersomes; Wound Healing - drug effects; Transfersomes; Gellan; SAXS analysis; Rheological studies; Skin delivery; In vivo studies
• ISSN: 1549-9634; 1549-9642
• DOI: 10.1016/j.nano.2017.12.001

Gellan nanohydrogel and phospholipid vesicles were combined to incorporate baicalin in new self-assembling core-shell gellan-transfersomes obtained by an easy, scalable method. The vesicles were small in size (~107 nm) and monodispersed (P.I. ≤ 0.24), forming a viscous system (~24 mPa/s) as compared to transfersomes (~1.6 mPa/s), as confirmed by rheological studies. Gellan was anchored to the bilayer domains through cholesterol, and the polymer chains were distributed onto the outer surface of the bilayer, thus forming a core-shell structure, as suggested by SAXS analyses. The optimal carrier ability of core-shell gellan-transfersomes was established by the high deposition of baicalin in the skin (~11% in the whole skin), especially in the deeper tissue (~8% in the dermis). Moreover, their ability to improve baicalin efficacy in anti-inflammatory and skin repair tests was confirmed in vivo in mice, providing the complete skin restoration and inhibiting all the studied inflammatory markers. Baicalin was loaded in new vesicular carrier designed to optimize its topical delivery. The polyphenol was incorporated in transferosomes and then, considering the advantages given by the association of phospholipid vesicles and hydrogels, they were combined with a gellan-cholesterol derivative to produce self-assembling core-shell gellan-transfersomes. These systems provided the greatest baicalin in vitro deposition in intact skin, thanks to their peculiar assembling structure, and appeared as promising formulations capable of maximizing the polyphenol protective effect on inflamed skin, allowing complete skin repair. [Display omitted]