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...
Main Authors: | , , , |
---|---|
Format: | Article |
Language: | English |
Published: |
Dove Medical Press
2016-06-01
|
Series: | International Journal of Nanomedicine |
Subjects: | |
Online Access: | https://www.dovepress.com/development-of-transmucosal-patch-loaded-with-anesthetic-and-analgesic-peer-reviewed-article-IJN |
id |
doaj-7788ba8b617647f7991f110dbb88e1cf |
---|---|
record_format |
Article |
spelling |
doaj-7788ba8b617647f7991f110dbb88e1cf2020-11-25T00:47:25ZengDove Medical PressInternational Journal of Nanomedicine1178-20132016-06-012016default2901292027521Development of transmucosal patch loaded with anesthetic and analgesic for dental procedures and in vivo evaluationNidhi MPatro MNKusumvalli SKusumdevi VMalviya 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, histopathologyhttps://www.dovepress.com/development-of-transmucosal-patch-loaded-with-anesthetic-and-analgesic-peer-reviewed-article-IJNsolid lipid nanoparticleBox-Behnken designtransmucosal patchPKPDCaco 2 permeabilityhistopathology |
collection |
DOAJ |
language |
English |
format |
Article |
sources |
DOAJ |
author |
Nidhi M Patro MN Kusumvalli S Kusumdevi V |
spellingShingle |
Nidhi M Patro MN Kusumvalli S Kusumdevi V Development of transmucosal patch loaded with anesthetic and analgesic for dental procedures and in vivo evaluation International Journal of Nanomedicine solid lipid nanoparticle Box-Behnken design transmucosal patch PKPD Caco 2 permeability histopathology |
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 |
series |
International Journal of Nanomedicine |
issn |
1178-2013 |
publishDate |
2016-06-01 |
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 |
topic |
solid lipid nanoparticle Box-Behnken design transmucosal patch PKPD Caco 2 permeability histopathology |
url |
https://www.dovepress.com/development-of-transmucosal-patch-loaded-with-anesthetic-and-analgesic-peer-reviewed-article-IJN |
work_keys_str_mv |
AT nidhim developmentoftransmucosalpatchloadedwithanestheticandanalgesicfordentalproceduresandinvivoevaluation AT patromn developmentoftransmucosalpatchloadedwithanestheticandanalgesicfordentalproceduresandinvivoevaluation AT kusumvallis developmentoftransmucosalpatchloadedwithanestheticandanalgesicfordentalproceduresandinvivoevaluation AT kusumdeviv developmentoftransmucosalpatchloadedwithanestheticandanalgesicfordentalproceduresandinvivoevaluation |
_version_ |
1725260008258535424 |