A pre-formulation study of tetracaine loaded in optimized nanostructured lipid carriers

Abstract Tetracaine (TTC) is a local anesthetic broadly used for topical and spinal blockade, despite its systemic toxicity. Encapsulation in nanostructured lipid carriers (NLC) may prolong TTC delivery at the site of injection, reducing such toxicity. This work reports the development of NLC loadin...

Descripción completa

Guardado en:

Detalles Bibliográficos
Autores principales:	Simone R. Castro, Lígia N. M. Ribeiro, Márcia C. Breitkreitz, Viviane A. Guilherme, Gustavo H. Rodrigues da Silva, Hery Mitsutake, Ana C. S. Alcântara, Fabiano Yokaichiya, Margareth K. K. D. Franco, Daniel Clemens, Ben Kent, Marcelo Lancellotti, Daniele R. de Araújo, Eneida de Paula
Formato:	article
Lenguaje:	EN
Publicado:	Nature Portfolio 2021
Materias:	Medicine R Science Q
Acceso en línea:	https://doaj.org/article/2a392a9650a24606a11c70d5ae2df5f8
Etiquetas:	Agregar Etiqueta Sin Etiquetas, Sea el primero en etiquetar este registro!

id	oai:doaj.org-article:2a392a9650a24606a11c70d5ae2df5f8
record_format	dspace
spelling	oai:doaj.org-article:2a392a9650a24606a11c70d5ae2df5f82021-11-08T10:55:48ZA pre-formulation study of tetracaine loaded in optimized nanostructured lipid carriers10.1038/s41598-021-99743-62045-2322https://doaj.org/article/2a392a9650a24606a11c70d5ae2df5f82021-11-01T00:00:00Zhttps://doi.org/10.1038/s41598-021-99743-6https://doaj.org/toc/2045-2322Abstract Tetracaine (TTC) is a local anesthetic broadly used for topical and spinal blockade, despite its systemic toxicity. Encapsulation in nanostructured lipid carriers (NLC) may prolong TTC delivery at the site of injection, reducing such toxicity. This work reports the development of NLC loading 4% TTC. Structural properties and encapsulation efficiency (%EE > 63%) guided the selection of three pre-formulations of different lipid composition, through a 23 factorial design of experiments (DOE). DLS and TEM analyses revealed average sizes (193–220 nm), polydispersity (< 0.2), zeta potential \|− 21.8 to − 30.1 mV\| and spherical shape of the nanoparticles, while FTIR-ATR, NTA, DSC, XRD and SANS provided details on their structure and physicochemical stability over time. Interestingly, one optimized pre-formulation (CP-TRANS/TTC) showed phase-separation after 4 months, as predicted by Raman imaging that detected lack of miscibility between its solid (cetyl palmitate) and liquid (Transcutol) lipids. SANS analyses identified lamellar arrangements inside such nanoparticles, the thickness of the lamellae been decreased by TTC. As a result of this combined approach (DOE and biophysical techniques) two optimized pre-formulations were rationally selected, both with great potential as drug delivery systems, extending the release of the anesthetic (> 48 h) and reducing TTC cytotoxicity against Balb/c 3T3 cells.Simone R. CastroLígia N. M. RibeiroMárcia C. BreitkreitzViviane A. GuilhermeGustavo H. Rodrigues da SilvaHery MitsutakeAna C. S. AlcântaraFabiano YokaichiyaMargareth K. K. D. FrancoDaniel ClemensBen KentMarcelo LancellottiDaniele R. de AraújoEneida de PaulaNature PortfolioarticleMedicineRScienceQENScientific Reports, Vol 11, Iss 1, Pp 1-15 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine R Science Q
spellingShingle	Medicine R Science Q Simone R. Castro Lígia N. M. Ribeiro Márcia C. Breitkreitz Viviane A. Guilherme Gustavo H. Rodrigues da Silva Hery Mitsutake Ana C. S. Alcântara Fabiano Yokaichiya Margareth K. K. D. Franco Daniel Clemens Ben Kent Marcelo Lancellotti Daniele R. de Araújo Eneida de Paula A pre-formulation study of tetracaine loaded in optimized nanostructured lipid carriers
description	Abstract Tetracaine (TTC) is a local anesthetic broadly used for topical and spinal blockade, despite its systemic toxicity. Encapsulation in nanostructured lipid carriers (NLC) may prolong TTC delivery at the site of injection, reducing such toxicity. This work reports the development of NLC loading 4% TTC. Structural properties and encapsulation efficiency (%EE > 63%) guided the selection of three pre-formulations of different lipid composition, through a 23 factorial design of experiments (DOE). DLS and TEM analyses revealed average sizes (193–220 nm), polydispersity (< 0.2), zeta potential \|− 21.8 to − 30.1 mV\| and spherical shape of the nanoparticles, while FTIR-ATR, NTA, DSC, XRD and SANS provided details on their structure and physicochemical stability over time. Interestingly, one optimized pre-formulation (CP-TRANS/TTC) showed phase-separation after 4 months, as predicted by Raman imaging that detected lack of miscibility between its solid (cetyl palmitate) and liquid (Transcutol) lipids. SANS analyses identified lamellar arrangements inside such nanoparticles, the thickness of the lamellae been decreased by TTC. As a result of this combined approach (DOE and biophysical techniques) two optimized pre-formulations were rationally selected, both with great potential as drug delivery systems, extending the release of the anesthetic (> 48 h) and reducing TTC cytotoxicity against Balb/c 3T3 cells.
format	article
author	Simone R. Castro Lígia N. M. Ribeiro Márcia C. Breitkreitz Viviane A. Guilherme Gustavo H. Rodrigues da Silva Hery Mitsutake Ana C. S. Alcântara Fabiano Yokaichiya Margareth K. K. D. Franco Daniel Clemens Ben Kent Marcelo Lancellotti Daniele R. de Araújo Eneida de Paula
author_facet	Simone R. Castro Lígia N. M. Ribeiro Márcia C. Breitkreitz Viviane A. Guilherme Gustavo H. Rodrigues da Silva Hery Mitsutake Ana C. S. Alcântara Fabiano Yokaichiya Margareth K. K. D. Franco Daniel Clemens Ben Kent Marcelo Lancellotti Daniele R. de Araújo Eneida de Paula
author_sort	Simone R. Castro
title	A pre-formulation study of tetracaine loaded in optimized nanostructured lipid carriers
title_short	A pre-formulation study of tetracaine loaded in optimized nanostructured lipid carriers
title_full	A pre-formulation study of tetracaine loaded in optimized nanostructured lipid carriers
title_fullStr	A pre-formulation study of tetracaine loaded in optimized nanostructured lipid carriers
title_full_unstemmed	A pre-formulation study of tetracaine loaded in optimized nanostructured lipid carriers
title_sort	pre-formulation study of tetracaine loaded in optimized nanostructured lipid carriers
publisher	Nature Portfolio
publishDate	2021
url	https://doaj.org/article/2a392a9650a24606a11c70d5ae2df5f8
work_keys_str_mv	AT simonercastro apreformulationstudyoftetracaineloadedinoptimizednanostructuredlipidcarriers AT ligianmribeiro apreformulationstudyoftetracaineloadedinoptimizednanostructuredlipidcarriers AT marciacbreitkreitz apreformulationstudyoftetracaineloadedinoptimizednanostructuredlipidcarriers AT vivianeaguilherme apreformulationstudyoftetracaineloadedinoptimizednanostructuredlipidcarriers AT gustavohrodriguesdasilva apreformulationstudyoftetracaineloadedinoptimizednanostructuredlipidcarriers AT herymitsutake apreformulationstudyoftetracaineloadedinoptimizednanostructuredlipidcarriers AT anacsalcantara apreformulationstudyoftetracaineloadedinoptimizednanostructuredlipidcarriers AT fabianoyokaichiya apreformulationstudyoftetracaineloadedinoptimizednanostructuredlipidcarriers AT margarethkkdfranco apreformulationstudyoftetracaineloadedinoptimizednanostructuredlipidcarriers AT danielclemens apreformulationstudyoftetracaineloadedinoptimizednanostructuredlipidcarriers AT benkent apreformulationstudyoftetracaineloadedinoptimizednanostructuredlipidcarriers AT marcelolancellotti apreformulationstudyoftetracaineloadedinoptimizednanostructuredlipidcarriers AT danielerdearaujo apreformulationstudyoftetracaineloadedinoptimizednanostructuredlipidcarriers AT eneidadepaula apreformulationstudyoftetracaineloadedinoptimizednanostructuredlipidcarriers AT simonercastro preformulationstudyoftetracaineloadedinoptimizednanostructuredlipidcarriers AT ligianmribeiro preformulationstudyoftetracaineloadedinoptimizednanostructuredlipidcarriers AT marciacbreitkreitz preformulationstudyoftetracaineloadedinoptimizednanostructuredlipidcarriers AT vivianeaguilherme preformulationstudyoftetracaineloadedinoptimizednanostructuredlipidcarriers AT gustavohrodriguesdasilva preformulationstudyoftetracaineloadedinoptimizednanostructuredlipidcarriers AT herymitsutake preformulationstudyoftetracaineloadedinoptimizednanostructuredlipidcarriers AT anacsalcantara preformulationstudyoftetracaineloadedinoptimizednanostructuredlipidcarriers AT fabianoyokaichiya preformulationstudyoftetracaineloadedinoptimizednanostructuredlipidcarriers AT margarethkkdfranco preformulationstudyoftetracaineloadedinoptimizednanostructuredlipidcarriers AT danielclemens preformulationstudyoftetracaineloadedinoptimizednanostructuredlipidcarriers AT benkent preformulationstudyoftetracaineloadedinoptimizednanostructuredlipidcarriers AT marcelolancellotti preformulationstudyoftetracaineloadedinoptimizednanostructuredlipidcarriers AT danielerdearaujo preformulationstudyoftetracaineloadedinoptimizednanostructuredlipidcarriers AT eneidadepaula preformulationstudyoftetracaineloadedinoptimizednanostructuredlipidcarriers
_version_	1718442506736107520

A pre-formulation study of tetracaine loaded in optimized nanostructured lipid carriers

Ejemplares similares