Development of transmucosal patch loaded with anesthetic and analgesic for dental procedures and in vivo evaluation

Malviya Nidhi,1 M Nagaraju Patro,1 Somisetty Kusumvalli,2 Vemula Kusumdevi1 1Department of Pharmaceutics, Al-Ameen College of Pharmacy, 2Department of Endodontics and Conservative Dentistry, Sri Rajiv Gandhi College of Dental Sciences, Bengaluru, Karnataka, India Abstract: Most of the dental surge...

Descripción completa

Guardado en:
Detalles Bibliográficos
Autores principales: Nidhi M, Patro MN, Kusumvalli S, Kusumdevi V
Formato: article
Lenguaje:EN
Publicado: Dove Medical Press 2016
Materias:
Acceso en línea:https://doaj.org/article/7788ba8b617647f7991f110dbb88e1cf
Etiquetas: Agregar Etiqueta
Sin Etiquetas, Sea el primero en etiquetar este registro!
id oai:doaj.org-article:7788ba8b617647f7991f110dbb88e1cf
record_format dspace
spelling oai:doaj.org-article:7788ba8b617647f7991f110dbb88e1cf2021-12-02T03:58:38ZDevelopment of transmucosal patch loaded with anesthetic and analgesic for dental procedures and in vivo evaluation1178-2013https://doaj.org/article/7788ba8b617647f7991f110dbb88e1cf2016-06-01T00:00:00Zhttps://www.dovepress.com/development-of-transmucosal-patch-loaded-with-anesthetic-and-analgesic-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Malviya Nidhi,1 M Nagaraju Patro,1 Somisetty Kusumvalli,2 Vemula Kusumdevi1 1Department of Pharmaceutics, Al-Ameen College of Pharmacy, 2Department of Endodontics and Conservative Dentistry, Sri Rajiv Gandhi College of Dental Sciences, Bengaluru, Karnataka, India Abstract: Most of the dental surgeries require preoperative anesthetic and postoperative analgesic for painless procedures. A multidrug transmucosal drug delivery system loaded with lignocaine (Lig) base for immediate release and solid lipid nanoparticles (SLNs) of diclofenac (Dic) diethylamine for prolonged release was developed. SLNs were prepared by solvent emulsion–evaporation method with Precirol ATO 5 and Geleol as lipids and Pluronic F 68 as surfactant and optimized with Box–Behnken design for particle size and entrapment efficiency. SLNs were incorporated into the transmucosal patch (TP) prepared with hydroxypropyl cellulose-LF (HPC-LF) and with a backing layer of ethyl cellulose. Optimized SLNs and TP were characterized for Fourier transform infrared spectrophotometry, differential scanning calorimetry, scanning electron microscopy, X-ray diffraction, in vitro release, ex vivo permeation through porcine buccal mucosa, Caco-2 permeability, and residual solvent analysis by gas chromatography. The TP was also evaluated for swelling index, in vitro residence time, tensile strength, and mucoadhesive strength. Preclinical pharmacokinetic, pharmacodynamic, and histopathological studies by application of TP on the gingiva of New Zealand rabbits were carried out. Particle size and entrapment efficiency of the optimized SLN “S8” were determined as 98.23 nm and 84.36%, respectively. The gingival crevicular fluid and tissue concentrations were greater than plasma concentrations with increase in Cmax and area under the curve (AUC) of Lig and Dic when compared to the control group. Pain perception by needle prick showed prolonged combined anesthetic and analgesic effect. The developed TP loaded with Lig base and Dic diethylamine-SLNs exhibited immediate and complete permeation with tissue accumulation of Lig followed by controlled prolonged release and tissue accumulation of Dic at the site of application. Thus, it could be anticipated from the in vivo studies that the developed TP provides immediate initial anesthetic effect, and the analgesic effect would be prolonged for 24 hours, since optimal gingival crevicular fluid and tissue levels of analgesic would be achieved, while the tissue remains anesthetized. Keywords: solid lipid nanoparticle, Box–Behnken design, transmucosal patch, pharmacokinetics and pharmacodynamics, Caco-2 permeability, histopathologyNidhi MPatro MNKusumvalli SKusumdevi VDove Medical Pressarticlesolid lipid nanoparticleBox-Behnken designtransmucosal patchPKPDCaco 2 permeabilityhistopathologyMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2016, Iss default, Pp 2901-2920 (2016)
institution DOAJ
collection DOAJ
language EN
topic solid lipid nanoparticle
Box-Behnken design
transmucosal patch
PKPD
Caco 2 permeability
histopathology
Medicine (General)
R5-920
spellingShingle solid lipid nanoparticle
Box-Behnken design
transmucosal patch
PKPD
Caco 2 permeability
histopathology
Medicine (General)
R5-920
Nidhi M
Patro MN
Kusumvalli S
Kusumdevi V
Development of transmucosal patch loaded with anesthetic and analgesic for dental procedures and in vivo evaluation
description Malviya Nidhi,1 M Nagaraju Patro,1 Somisetty Kusumvalli,2 Vemula Kusumdevi1 1Department of Pharmaceutics, Al-Ameen College of Pharmacy, 2Department of Endodontics and Conservative Dentistry, Sri Rajiv Gandhi College of Dental Sciences, Bengaluru, Karnataka, India Abstract: Most of the dental surgeries require preoperative anesthetic and postoperative analgesic for painless procedures. A multidrug transmucosal drug delivery system loaded with lignocaine (Lig) base for immediate release and solid lipid nanoparticles (SLNs) of diclofenac (Dic) diethylamine for prolonged release was developed. SLNs were prepared by solvent emulsion–evaporation method with Precirol ATO 5 and Geleol as lipids and Pluronic F 68 as surfactant and optimized with Box–Behnken design for particle size and entrapment efficiency. SLNs were incorporated into the transmucosal patch (TP) prepared with hydroxypropyl cellulose-LF (HPC-LF) and with a backing layer of ethyl cellulose. Optimized SLNs and TP were characterized for Fourier transform infrared spectrophotometry, differential scanning calorimetry, scanning electron microscopy, X-ray diffraction, in vitro release, ex vivo permeation through porcine buccal mucosa, Caco-2 permeability, and residual solvent analysis by gas chromatography. The TP was also evaluated for swelling index, in vitro residence time, tensile strength, and mucoadhesive strength. Preclinical pharmacokinetic, pharmacodynamic, and histopathological studies by application of TP on the gingiva of New Zealand rabbits were carried out. Particle size and entrapment efficiency of the optimized SLN “S8” were determined as 98.23 nm and 84.36%, respectively. The gingival crevicular fluid and tissue concentrations were greater than plasma concentrations with increase in Cmax and area under the curve (AUC) of Lig and Dic when compared to the control group. Pain perception by needle prick showed prolonged combined anesthetic and analgesic effect. The developed TP loaded with Lig base and Dic diethylamine-SLNs exhibited immediate and complete permeation with tissue accumulation of Lig followed by controlled prolonged release and tissue accumulation of Dic at the site of application. Thus, it could be anticipated from the in vivo studies that the developed TP provides immediate initial anesthetic effect, and the analgesic effect would be prolonged for 24 hours, since optimal gingival crevicular fluid and tissue levels of analgesic would be achieved, while the tissue remains anesthetized. Keywords: solid lipid nanoparticle, Box–Behnken design, transmucosal patch, pharmacokinetics and pharmacodynamics, Caco-2 permeability, histopathology
format article
author Nidhi M
Patro MN
Kusumvalli S
Kusumdevi V
author_facet Nidhi M
Patro MN
Kusumvalli S
Kusumdevi V
author_sort Nidhi M
title Development of transmucosal patch loaded with anesthetic and analgesic for dental procedures and in vivo evaluation
title_short Development of transmucosal patch loaded with anesthetic and analgesic for dental procedures and in vivo evaluation
title_full Development of transmucosal patch loaded with anesthetic and analgesic for dental procedures and in vivo evaluation
title_fullStr Development of transmucosal patch loaded with anesthetic and analgesic for dental procedures and in vivo evaluation
title_full_unstemmed Development of transmucosal patch loaded with anesthetic and analgesic for dental procedures and in vivo evaluation
title_sort development of transmucosal patch loaded with anesthetic and analgesic for dental procedures and in vivo evaluation
publisher Dove Medical Press
publishDate 2016
url https://doaj.org/article/7788ba8b617647f7991f110dbb88e1cf
work_keys_str_mv AT nidhim developmentoftransmucosalpatchloadedwithanestheticandanalgesicfordentalproceduresandinvivoevaluation
AT patromn developmentoftransmucosalpatchloadedwithanestheticandanalgesicfordentalproceduresandinvivoevaluation
AT kusumvallis developmentoftransmucosalpatchloadedwithanestheticandanalgesicfordentalproceduresandinvivoevaluation
AT kusumdeviv developmentoftransmucosalpatchloadedwithanestheticandanalgesicfordentalproceduresandinvivoevaluation
_version_ 1718401497653313536