Pre-clinical validation of a vaginal cream containing copaiba oil (reproductive toxicology study)

Abstract

The aims of this study was to evaluate the effects of oil-resin of Copaiba (Copaifera duckei Dwyer), aired in vaginal cream on the reproductive performance of female rats (Rattus norvegicus). To determine the components of the C. duckei oleoresin, gas chromatography coupled with mass spectrometry (CG-MS) was used, and considering the trans-caryophyllene sesquiterpene as a phytochemical marker in the oleoresin. Due to the extensive use of copaiba oleoresin in the suppository form for gynecological infections, an evaluation was carried out on the effects of copaiba oleoresin (Copaifera duckei Dwyer), delivered in a vaginal cream, on the reproductive performance of female Wistar rats. For this purpose, three groups (n=5-6/group) of female rats were treated as follows: 1--vaginal cream of copaiba oleoresin (28.6 mg/kg), 2--base vaginal cream and 3--control (physiological saline 0.9%), administered intravaginally, for 30 days before pregnancy, and from day zero to day 20 during pregnancy. Laparotomy was performed on the 21st day of pregnancy, followed by the determination of reproductive variables: number of live and dead fetuses, mass of the fetuses and placentas, number of implantations and resorptions, number of corpora lutea, pre- and post-implantation loss, and analyses of the fetuses with regard to external and internal anomalies and/or malformations (skeletal and visceral). The trans-caryophyllene present in the sample is suggested as a phytochemical marker and the results of this study demonstrate an absence of maternal toxicity and foetotoxicity embryofoetotoxicity at the dose administered, corresponding to ten times the recommended dose for use in humans. Accordingly, no significant statistical difference was observed between the treated and control groups, for the variables analyzed. Thus, it is concluded that the vaginal cream containing 2.5% copaiba oleoresin is safe during gestation, in female rats (Rattus norvegicus) of the Wistar strain.

Development of a larvicidal nanoemulsion with Copaiba (Copaifera duckei) oleoresin

“…Copaiba oleoresins are mainly constituted by sesquiterpene hydrocarbons, which often correspond to almost 90% of the total relative composition of the oil, being beta-caryophyllene considered the main constituent. Previous chemical characterization of the oleoresin used in the present study confirmed this profile (Lima et al, 2011). Diterpenes are also found in smaller quantities in copaiba oleoresin (Sousa et al, 2011).…”

Development and Validation of a Rapid and Reliable RP-HPLC-PDA Method for the Quantification of Six Diterpenes in Copaifera duckei, Copaifera reticulata and Copaifera multijuga Oleoresins

“…4,5,34 Despite their importance, many reports concerning the valuable properties of these balsams have not provided the proper botanical identification and/or a complete chemical characterization. As mentioned before, most of the previous reported studies had just carried out the chemical characterization of the volatile constituents, 2,[16][17][18][19][20] and have described the presence of more than 70 sesquiterpenes. 2,9,10,35 Despite the importance of sesquiterpenes on the chemical and biological characterization of Copaifera oleoresins, [1][2][3][17][18][19] recent reports have established that several non-volatile diterpenes, such as (-)-copalic acid, ent-kaurenoic acid and (-)-polyalthic acid, are also responsible for important biological properties displayed by these balsams.…”

“…As mentioned before, most of the previous reported studies had just carried out the chemical characterization of the volatile constituents, 2,[16][17][18][19][20] and have described the presence of more than 70 sesquiterpenes. 2,9,10,35 Despite the importance of sesquiterpenes on the chemical and biological characterization of Copaifera oleoresins, [1][2][3][17][18][19] recent reports have established that several non-volatile diterpenes, such as (-)-copalic acid, ent-kaurenoic acid and (-)-polyalthic acid, are also responsible for important biological properties displayed by these balsams. 3,11,12,14,15,22 Even though and as stated before, there are only two analytical methods to characterize these diterpene acids in Copaifera oleoresins.…”

“…Acid diterpenes stands out for a wide range of the biological properties reported for these oleoresins, such as: antimicrobial, antitumoral, antinociceptive and anti-inflammatory, among others. 3,4,6,[11][12][13][14][15] Despite this fact, most of the studies reporting the chemical identification and quantification of the diterpenes of Copaifera oleoresins have been performed by using gas chromatographic hyphenated techniques and mass spectra comparison with spectral libraries, 2,[16][17][18][19][20] which are more adequate for analyses of volatile compounds like sesquiterpenes. 9 In the literature, there are only two studies describing the development and validation of analytical methods for the analysis acid diterpenes 9,21 in Copaifera species.…”

Production of Phytotherapeutics in Brazil: History, Problems and Perspectives

“…Para Gândavo 49 ,antiinflamatória [261][262][263][264][265][266][267] , antileishmania [268][269][270][271] , na endometriose 272 , na urolitíase 273 , na acne 274 , na psoríase 275 , no controle do mosquito Aedes aegypti [276][277][278] , no controle de ácaros 279 e em infecções ginecológicas. 280 O óleo da copaíba também reduz os níveis séricos de ureia e creatinina em ratos submetidos à síndrome de isquemia e reperfusão. Deve-se notar que no rim, a lesão induzida por isquemia e reperfusão se constitui na principal causa da insuficiência renal aguda, que se caracteriza, entre outros aspectos, por uma elevação transitória na taxa de creatinina.…”