Phycocyanin liposomes for topical anti-inflammatory activity: in-vitro in-vivo studies.
OBJECTIVE
The aim of this work was to investigate the anti-inflammatory activity of C-phycocyanin (C-PC) on skin inflammation after topical administration and the influence of liposomal delivery on its pharmacokinetic properties.


METHODS
Liposomes of different size and structure were prepared with different techniques using soy phosphatidylcholine and cholesterol. Vesicular dispersions were characterised by transmission electron microscopy, optical and fluorescence microscopy for vesicle formation and morphology, dynamic laser light scattering for size distribution, and Zetasizer for zeta-potential. C-PC skin penetration and permeation experiments were performed in vitro using vertical diffusion Franz cells and human skin treated with either free or liposomal drug dispersed in a Carbopol gel.


RESULTS
The protein was mainly localised in the stratum corneum, while no permeation of C-PC through the whole skin thickness was detected. Two percent C-PC-encapsulating liposomes showed the best drug accumulation in the stratum corneum and the whole skin, higher than that of the corresponding free 2% C-PC gel. Moreover, skin deposition of liposomal C-PC was dose dependent since skin accumulation values increased as the C-PC concentration in liposomes increased. The topical anti-inflammatory activity of samples was evaluated in vivo as inhibition of croton oil-induced or arachidonic acid-induced ear oedema in rats.


CONCLUSIONS
The results showed that C-PC can be successfully used as an anti-inflammatory drug and that liposomal encapsulation is effective in improving its anti-inflammatory activity.
Manconia
Maria
M
Dipartimento Farmaco Chimico Tecnologico, Universitá di Cagliari, Cagliari, Italy.
Pendás
Jehzabel
J
Ledón
Nurys
N
Moreira
Tomás
T
Sinico
Chiara
C
Saso
Luciano
L
Fadda
Anna Maria
AM
D000279:Administration, Cutaneous; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000627:therapeutic use*; D016718:Arachidonic Acid; D003436:Croton Oil; D016503:Drug Delivery Systems / Q000379:methods; D004423:Ear; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy*; D006801:Humans; D066298:In Vitro Techniques; D008081:Liposomes; D008297:Male; D010798:Phycocyanin / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000627:therapeutic use*; D051381:Rats; D012867:Skin / Q000378:metabolism; D012869:Skin Absorption
D000893:Anti-Inflammatory Agents; D008081:Liposomes; D010798:Phycocyanin; D016718:Arachidonic Acid; D003436:Croton Oil