PMID- 25303852 OWN - NLM STAT- MEDLINE DCOM- 20150819 LR - 20220321 IS - 1873-4367 (Electronic) IS - 0927-7765 (Linking) VI - 123 DP - 2014 Nov 1 TI - Physicochemical characterization of epigallocatechin gallate lipid nanoparticles (EGCG-LNs) for ocular instillation. PG - 452-60 LID - S0927-7765(14)00513-X [pii] LID - 10.1016/j.colsurfb.2014.09.042 [doi] 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. CI - Copyright (c) 2014 Elsevier B.V. All rights reserved. FAU - Fangueiro, Joana F AU - Fangueiro JF AD - CEBIMED, Research Centre for Biomedicine, Fernando Pessoa University, UFP-FCS, Praca 9 de Abril, 349, P-4249-004 Porto, Portugal; Faculty of Health Sciences, Fernando Pessoa University, UFP-FCS, Rua Carlos da Maia, 296, 4200-150 Porto, Portugal. FAU - Andreani, Tatiana AU - Andreani T AD - Faculty of Health Sciences, Fernando Pessoa University, UFP-FCS, Rua Carlos da Maia, 296, 4200-150 Porto, Portugal; Centre for Research and Technology of Agro-Environmental and Biological Sciences, CITAB, University of Tras-os-Montes e Alto Douro, UTAD, Quinta de Prados, 5000-801 Vila Real, Portugal; Department of Biology and Environment, University of Tras-os-Montes e Alto Douro, UTAD, Quinta de Prados, 5000-801 Vila Real, Portugal. FAU - Fernandes, Lisete AU - Fernandes L AD - Electron Microscopy Unit, University of Tras-os-Montes e Alto Douro, UTAD, Quinta de Prados, 5000-801 Vila Real, Portugal. FAU - Garcia, Maria L AU - Garcia ML AD - Department of Physical Chemistry, Faculty of Pharmacy, University of Barcelona, Av. Joan XXIII s/n, 08028 Barcelona, Spain; Institute of Nanoscience and Nanotechnology, University of Barcelona, Av. Joan XXIII s/n, 08028 Barcelona, Spain. FAU - Egea, Maria A AU - Egea MA AD - Department of Physical Chemistry, Faculty of Pharmacy, University of Barcelona, Av. Joan XXIII s/n, 08028 Barcelona, Spain; Institute of Nanoscience and Nanotechnology, University of Barcelona, Av. Joan XXIII s/n, 08028 Barcelona, Spain. FAU - Silva, Amelia M AU - Silva AM AD - Centre for Research and Technology of Agro-Environmental and Biological Sciences, CITAB, University of Tras-os-Montes e Alto Douro, UTAD, Quinta de Prados, 5000-801 Vila Real, Portugal; Department of Biology and Environment, University of Tras-os-Montes e Alto Douro, UTAD, Quinta de Prados, 5000-801 Vila Real, Portugal. FAU - Souto, Eliana B AU - Souto EB AD - CEBIMED, Research Centre for Biomedicine, Fernando Pessoa University, UFP-FCS, Praca 9 de Abril, 349, P-4249-004 Porto, Portugal; Faculty of Pharmacy of University of Coimbra (FFUC), Polo das Ciencias da Saude, Azinhaga de Santa Comba, 3000-548 Coimbra, Portugal. Electronic address: ebsouto@ff.uc.pt. LA - eng PT - Journal Article PT - Research Support, Non-U.S. Gov't DEP - 20140928 PL - Netherlands TA - Colloids Surf B Biointerfaces JT - Colloids and surfaces. B, Biointerfaces JID - 9315133 RN - 0 (Cetrimonium Compounds) RN - 0 (Drug Carriers) RN - 0 (Lipids) RN - 0 (Quaternary Ammonium Compounds) RN - 0 (dimethyldinonylammonium bromide) RN - 8R1V1STN48 (Catechin) RN - BQM438CTEL (epigallocatechin gallate) RN - Z7FF1XKL7A (Cetrimonium) SB - IM MH - Administration, Ophthalmic MH - Catechin/*analogs & derivatives/chemistry MH - Cetrimonium MH - Cetrimonium Compounds/chemistry MH - Drug Carriers/chemistry MH - Humans MH - Lipids/*chemistry MH - Nanoparticles/*chemistry MH - Quaternary Ammonium Compounds/chemistry OTO - NOTNLM OT - Catechins OT - Cationic lipid OT - Epigallocatechin gallate OT - Lipid nanoparticles OT - Multiple emulsion OT - Ocular delivery EDAT- 2014/10/12 06:00 MHDA- 2015/08/20 06:00 CRDT- 2014/10/12 06:00 PHST- 2014/05/16 00:00 [received] PHST- 2014/08/04 00:00 [revised] PHST- 2014/09/19 00:00 [accepted] PHST- 2014/10/12 06:00 [entrez] PHST- 2014/10/12 06:00 [pubmed] PHST- 2015/08/20 06:00 [medline] AID - S0927-7765(14)00513-X [pii] AID - 10.1016/j.colsurfb.2014.09.042 [doi] PST - ppublish SO - Colloids Surf B Biointerfaces. 2014 Nov 1;123:452-60. doi: 10.1016/j.colsurfb.2014.09.042. Epub 2014 Sep 28.