TY - JOUR
T1 - Physicochemical characterization of epigallocatechin gallate lipid nanoparticles (EGCG-LNs) for ocular instillation
AU - Fangueiro, Joana F.
AU - Andreani, Tatiana
AU - Fernandes, Lisete
AU - Garcia, Maria L.
AU - Egea, Maria A.
AU - Silva, Amélia M.
AU - Souto, Eliana B.
N1 - Funding Information:
Ms. Joana Fangueiro and Ms. Tatiana Andreani wish to acknowledge Fundação para a Ciência e Tecnologia do Ministério da Ciência e Tecnologia (FCT, Portugal) under the references SFRH/BD/80335/2011 and SFRH/BD/60640/2009 , respectively. FCT and European Funds (FEDER and COMPETE) are also acknowledged under the research project PTDC/SAU-FAR/113100/2009 and FCOMP-01-0124-FEDER-022696 (PEst-C/AGR/UI4033/2011) . The Subprograma de Proyectos de Investigación Fundamental no Orientada del Ministerio de Ciencia e Innovación is also acknowledged under the reference MAT2011-26994 .
Publisher Copyright:
© 2014 Elsevier B.V.
PY - 2014/9/28
Y1 - 2014/9/28
N2 - The encapsulation of epigallocatechin gallate (EGCG) in lipid nanoparticles (LNs) could be a suitable approach to avoid drug oxidation and epimerization, which are common processes that lead to low bioavailability of the drug limiting its therapeutic efficacy. The human health benefits of EGCG gained much interest in the pharmaceutical field, and so far there are no studies reporting its encapsulation in LNs. The purpose of this study has been the development of an innovative system for the ocular delivery of EGCG using LNs as carrier for the future treatment of several diseases, such as dry eye, age-related macular degeneration (AMD), glaucoma, diabetic retinopathy and macular oedema. LNs dispersions have been produced by multiple emulsion technique and previously optimized by a factorial design. In order to increase ocular retention time and mucoadhesion by electrostatic attraction, two distinct cationic lipids were used, namely, cetyltrimethylammonium bromide (CTAB) and dimethyldioctadecylammonium bromide (DDAB). EGCG has been successfully loaded in the LNs dispersions and the nanoparticles analysis over 30 days of storage time predicted a good physicochemical stability. The particles were found to be in the nanometer range (<300. nm) and all the evaluated parameters, namely pH, osmolarity and viscosity, were compatible to the ocular administration. The evaluation of the cationic lipid used was compared regarding physical and chemical parameters, lipid crystallization and polymorphism, and stability of dispersion during storage. The results show that different lipids lead to different characteristics mainly associated with the acyl chain composition, i.e. double lipid shows to have influence in the crystallization and stability. Despite the recorded differences between DTAB and DDAB, both cationic LNs seem to fit the parameters for ocular drug delivery.
AB - The encapsulation of epigallocatechin gallate (EGCG) in lipid nanoparticles (LNs) could be a suitable approach to avoid drug oxidation and epimerization, which are common processes that lead to low bioavailability of the drug limiting its therapeutic efficacy. The human health benefits of EGCG gained much interest in the pharmaceutical field, and so far there are no studies reporting its encapsulation in LNs. The purpose of this study has been the development of an innovative system for the ocular delivery of EGCG using LNs as carrier for the future treatment of several diseases, such as dry eye, age-related macular degeneration (AMD), glaucoma, diabetic retinopathy and macular oedema. LNs dispersions have been produced by multiple emulsion technique and previously optimized by a factorial design. In order to increase ocular retention time and mucoadhesion by electrostatic attraction, two distinct cationic lipids were used, namely, cetyltrimethylammonium bromide (CTAB) and dimethyldioctadecylammonium bromide (DDAB). EGCG has been successfully loaded in the LNs dispersions and the nanoparticles analysis over 30 days of storage time predicted a good physicochemical stability. The particles were found to be in the nanometer range (<300. nm) and all the evaluated parameters, namely pH, osmolarity and viscosity, were compatible to the ocular administration. The evaluation of the cationic lipid used was compared regarding physical and chemical parameters, lipid crystallization and polymorphism, and stability of dispersion during storage. The results show that different lipids lead to different characteristics mainly associated with the acyl chain composition, i.e. double lipid shows to have influence in the crystallization and stability. Despite the recorded differences between DTAB and DDAB, both cationic LNs seem to fit the parameters for ocular drug delivery.
KW - Catechins
KW - Cationic lipid
KW - Epigallocatechin gallate
KW - Lipid nanoparticles
KW - Multiple emulsion
KW - Ocular delivery
UR - http://www.scopus.com/inward/record.url?scp=84916208468&partnerID=8YFLogxK
U2 - 10.1016/j.colsurfb.2014.09.042
DO - 10.1016/j.colsurfb.2014.09.042
M3 - Article
AN - SCOPUS:84916208468
SN - 0927-7765
VL - 123
SP - 452
EP - 460
JO - Colloids and Surfaces B: Biointerfaces
JF - Colloids and Surfaces B: Biointerfaces
ER -