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1.
Biomed Pharmacother ; 91: 946-950, 2017 Jul.
Article in English | MEDLINE | ID: mdl-28514833

ABSTRACT

This study aimed to develop and to evaluate the antinociceptive effect of a drug delivery system containing (-)-α-bisabolol (BISA). Nanocapsules containing BISA (BISA-NC) were prepared using acetylated galatomannan. Particle size distribution was determined by atomic force microscopy, zeta potential measurement and photon correlation spectroscopy. Corneal nociception was induced by topical application of 5M NaCl and the nociceptive behavior was characterized by eye wiping in mice. Molecular docking was conducted on the TRPV1 channel. Nanocapsules showed mean particle sizes between 94.44 and 105.44nm and the zeta potential of was -1.34mV. Animals pretreated with BISA-NC (200mg/mL) had a significant reduction (**p<0.01) in the number of nociceptive behaviors. Docking study indicated an interaction between BISA and TRPV1. This study indicates that BISA-NC may be useful for producing eye drops for the treatment of ocular pain.


Subject(s)
Analgesics/pharmacology , Nanocapsules/administration & dosage , Nociception/drug effects , Sesquiterpenes/pharmacology , Animals , Disease Models, Animal , Drug Delivery Systems/methods , Mice , Monocyclic Sesquiterpenes , Ophthalmic Solutions/pharmacology , Particle Size
2.
Naunyn Schmiedebergs Arch Pharmacol ; 390(2): 187-195, 2017 Feb.
Article in English | MEDLINE | ID: mdl-27900410

ABSTRACT

The purposes of this study were to evaluate the anti-nociceptive effect of oral and topical administration of (-)-α-bisabolol (BISA) in rodent models of formalin- or cinnamaldehyde-induced orofacial pain and to explore the inhibitory mechanisms involved. Orofacial pain was induced by injecting 1.5% formalin into the upper lip of mice (20 µL) or into the temporomandibular joint (TMJ) of rats (50 µL). In another experiment, orofacial pain was induced with cinnamaldehyde (13.2 µg/lip). Nociceptive behavior was proxied by time (s) spent rubbing the injected area and by the incidence of head flinching. BISA (100, 200, or 400 mg/kg p.o. or 50, 100, or 200 mg/mL topical) or vehicle was administered 60 min before pain induction. The two formulations (lotion and syrup) were compared with regard to efficacy. The effect of BISA remained after incorporation into the formulations, and nociceptive behavior decreased significantly in all tests. The high binding affinity observed for BISA and TRPA1 in the molecular docking study was supported by in vivo experiments in which HC-030031 (a TRPA1 receptor antagonist) attenuated pain in a manner qualitatively and quantitatively similar to that of BISA. Blockers of opioid receptors, NO synthesis, and K+ ATP channels did not affect orofacial pain, nor inhibit the effect of BISA. In conclusion, BISA had a significant anti-nociceptive effect on orofacial pain. The effect may in part be due to TRPA1 antagonism. The fact that the effect of BISA remained after incorporation into oral and topical formulations suggests that the compound may be a useful adjuvant in the treatment of orofacial pain.


Subject(s)
Analgesics/pharmacology , Behavior, Animal/drug effects , Facial Pain/prevention & control , Nociception/drug effects , Nociceptive Pain/prevention & control , Sesquiterpenes/pharmacology , Temporomandibular Joint/drug effects , Acrolein/analogs & derivatives , Administration, Oral , Administration, Topical , Analgesics/administration & dosage , Analgesics/chemistry , Analgesics/metabolism , Animals , Binding Sites , Disease Models, Animal , Dose-Response Relationship, Drug , Drug Compounding , Facial Pain/chemically induced , Facial Pain/physiopathology , Facial Pain/psychology , Formaldehyde , Male , Mice , Molecular Docking Simulation , Monocyclic Sesquiterpenes , Nociceptive Pain/chemically induced , Nociceptive Pain/physiopathology , Nociceptive Pain/psychology , Protein Binding , Protein Conformation , Rats, Wistar , Sesquiterpenes/administration & dosage , Sesquiterpenes/chemistry , Sesquiterpenes/metabolism , TRPA1 Cation Channel , TRPC Cation Channels/antagonists & inhibitors , TRPC Cation Channels/chemistry , TRPC Cation Channels/metabolism , Temporomandibular Joint/metabolism , Temporomandibular Joint/physiopathology , Transient Receptor Potential Channels/antagonists & inhibitors , Transient Receptor Potential Channels/chemistry , Transient Receptor Potential Channels/metabolism
3.
Indian J Dent Res ; 27(4): 364-369, 2016.
Article in English | MEDLINE | ID: mdl-27723631

ABSTRACT

BACKGROUND: Plaque-associated gingivitis is a prevalent disease and research in its treatment using herbal agents must be encouraged to verify which would be a useful addition to the current range or chemotherapeutic treatment options. AIMS: The aim of this study was to evaluate the clinical effect of a mouth rinse containing 10% Anacardium occidentale (AO) Linn., a typical plant commonly found in the Northeast Region of Brazil, on the reduction of plaque and gingivitis in comparison to a gold-standard chemotherapeutic agent. MATERIALS AND METHODS: Thirty normosystemic adult volunteers of both genders, who had a minimum of twenty natural teeth, aging between 18 and 32 years, were enrolled in this crossover, controlled, examiner-blind clinical study. They were randomly allocated into three groups: 10% AO Linn. (n = 10); 0.12% chlorhexidine digluconate (CLX, n = 10); or placebo (PB, n = 10). All volunteers were instructed to brush their teeth with a fluoridated dentifrice two times a day (12/12 h) and to rinse for 1 min with one of the mouthwashes (AO, CLX, or PB) 30 min after tooth brushing for 1 month. Plaque index (PLI) and gingival bleeding index (BLI) were recorded on days 0 and 30. Nonparametric Kruskal-Wallis and Wilcoxon tests (α = 0.05) were performed to evaluate statistical differences among groups. RESULTS: There was a significant reduction (P < 0.05) on plaque and gingivitis at day 30 just in CLX ([PLI = 0.47 ± 0.16; -30%]; [BLI = 0.15 ± 0.09; -55.8%]) and AO ([PLI = 0.49 ± 0.21; -31%]; [BLI = 0.13 ± 0.10; -56.6%]) groups, but no statistically significant difference was observed among them (P > 0.05). CONCLUSION: Mouthwash containing 10% AO was effective as an antiplaque and antigingivitis agent, in a similar manner that 0.12% CLX.


Subject(s)
Anacardium , Anti-Infective Agents, Local/therapeutic use , Dental Plaque/drug therapy , Gingivitis/drug therapy , Mouthwashes/therapeutic use , Oils, Volatile/therapeutic use , Plant Oils/therapeutic use , Adolescent , Adult , Chlorhexidine/analogs & derivatives , Chlorhexidine/therapeutic use , Cross-Over Studies , Female , Humans , Male , Treatment Outcome
4.
Indian J Dent Res ; 24(5): 533-6, 2013.
Article in English | MEDLINE | ID: mdl-24355949

ABSTRACT

AIM: The aim of this study was to evaluate the antiplaque effect of Lippia sidoides (LS) by in vivo investigation. MATERIALS AND METHODS: Ten healthy volunteers participated in a cross-over, double-blind clinical study, using a 3-day partial-mouth plaque accumulation model. The participants abolished any method of mechanical oral hygiene and they were randomly assigned initially to use just the following mouth rinses: Distilled water (negative control group), 0.12% chlorhexidine digluconate (positive control group) or 10% LS (test group). The plaque index was recorded in the six anterior upper teeth at the end of the trial and the one-way ANOVA and Bonferroni tests were used to estimate the difference among groups. RESULTS: The clinical results did show statistically significant difference among three groups (P < 0.05), favoring the positive control group and test group, however, no difference in efficacy was found between them (P > 0.05). CONCLUSIONS: The mouth rinses containing 0.12% chlorhexidine digluconate and 10% LS were equally able to inhibit plaque re-growth.


Subject(s)
Dental Plaque/prevention & control , Lippia/chemistry , Mouthwashes , Sodium Hypochlorite/pharmacology , Double-Blind Method , Enterococcus faecalis/drug effects , Humans
5.
Eur J Dent ; 7(1): 28-34, 2013 Jan.
Article in English | MEDLINE | ID: mdl-23408652

ABSTRACT

OBJECTIVE: This parallel controlled clinical trial evaluated the effect of a gel containing Lippia sidoides essential oil on plaque and gingivitis control. METHODS: Thirty patients (n=30) were randomly selected and allocated into three groups: Lippia sidoides (LS, n=10), chlorhexidine (CLX, n=10) or placebo (control, n=10). Plaque and bleeding index were recorded at baseline and after three months. All volunteers were instructed to brush with the gel three times a day throughout the experiment period. RESULTS: There was a significant reduction on plaque and gingivitis in the test groups (P<.05), but no statistically significant difference was observed between them (P>.05). CONCLUSION: A gel preparation containing 10% Lippia sidoides essential oil was an efficient herbal antiplaque and antigingivitis agent.

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