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

Nidhi M, Patro MN, Kusumvalli S, Kusumdevi V - Int J Nanomedicine (2016)

Bottom Line: The gingival crevicular fluid and tissue concentrations were greater than plasma concentrations with increase in C max 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.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.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, Al-Ameen College of Pharmacy.

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 C max 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.

No MeSH data available.


Related in: MedlinePlus

Pain score on categorical scale (mean value, n=6).
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f8-ijn-11-2901: Pain score on categorical scale (mean value, n=6).

Mentions: No response of pain exhibited as eye blink, head shake, or body shiver was shown until the sixth hour by any of the rabbits in case of group 1 that received the TP. Onset of anesthesia was considered as that time point of needle prick from the time of application of TP where the rabbits showed no response to pain. Depth of anesthesia was confirmed as the depth of the lancing device. Since the anesthetic effect was followed by analgesic effect, the duration of combined effect was considered as the duration between the time points of no pain perception to pain perception. Further, pain relief was judged on a 5-point categorical scale, where no response =0, eye blink =1, head shake =2, body vibrate =3, and any combination of response =4. Figure 8 shows the mean (n=6) response of the three groups. The positive control group that received the Lig gel and oral Dic exhibited eye blink or head shake or both from the second hour onward. Perception of pain exhibited as body shake was visible from initial time point of 2 minutes onward in the case of negative control that received no medication. Thus, the anesthetic effect existed for 1 hour when tissue Lig concentrations are also considered. Combined anesthetic and analgesic effect was seen until the sixth hour in group 1 that received the TP.


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

Nidhi M, Patro MN, Kusumvalli S, Kusumdevi V - Int J Nanomedicine (2016)

Pain score on categorical scale (mean value, n=6).
© Copyright Policy
Related In: Results  -  Collection

License 1 - License 2
Show All Figures
getmorefigures.php?uid=PMC4920237&req=5

f8-ijn-11-2901: Pain score on categorical scale (mean value, n=6).
Mentions: No response of pain exhibited as eye blink, head shake, or body shiver was shown until the sixth hour by any of the rabbits in case of group 1 that received the TP. Onset of anesthesia was considered as that time point of needle prick from the time of application of TP where the rabbits showed no response to pain. Depth of anesthesia was confirmed as the depth of the lancing device. Since the anesthetic effect was followed by analgesic effect, the duration of combined effect was considered as the duration between the time points of no pain perception to pain perception. Further, pain relief was judged on a 5-point categorical scale, where no response =0, eye blink =1, head shake =2, body vibrate =3, and any combination of response =4. Figure 8 shows the mean (n=6) response of the three groups. The positive control group that received the Lig gel and oral Dic exhibited eye blink or head shake or both from the second hour onward. Perception of pain exhibited as body shake was visible from initial time point of 2 minutes onward in the case of negative control that received no medication. Thus, the anesthetic effect existed for 1 hour when tissue Lig concentrations are also considered. Combined anesthetic and analgesic effect was seen until the sixth hour in group 1 that received the TP.

Bottom Line: The gingival crevicular fluid and tissue concentrations were greater than plasma concentrations with increase in C max 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.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.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, Al-Ameen College of Pharmacy.

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 C max 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.

No MeSH data available.


Related in: MedlinePlus