• Archives of Pharmacal Research
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• v.28 no.12
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• pp.1400-1404
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• 2005

The aim of the present study was to develop the aqueous parenteral formulation containing propofol using o/w microemulsion systems. Propofol itself was chosen as the oil phase and its content was fixed to 1$\%$, w/w. Pseudoternary phase diagrams were constructed to obtain the concentration range of surfactant and cosurfacatnt and the optimum ratio between them for microemulsion formation. Consequently, the suitability of the chosen microemulsion system as a parenteral formulation was evaluated from the stability and hemolysis tests on that. Among the surfactants and cosurfactants screened, the mixture of Solutol HS 15-ethyl alcohol (5/1) showed the largest o/w mocroemulsion region in the phase diagram. When 1 $\%$ (w/w) of propofol was solubilized with 8$\%$ (w/w) of Solutol $HS^{circledR}$??? 15-ethyl alcohol (5/1), the average droplet size (150 nm) and the content of propofol in the systems were not significantly changed at 40$^{circ}C$ for 8 weeks. The hemolysis test showed that this formulation was nontoxic to red blood cells. In conclusion, propofol was successfully solubilized with the o/w microemulsion systems.

• Journal of Dental Anesthesia and Pain Medicine
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• v.17 no.1
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• pp.21-28
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• 2017

Background: The skin consists of tightly connected keratinocytes, and prevents extensive water loss while simultaneously protecting against the entry of microbial pathogens. Excessive cellular levels of reactive oxygen species can induce cell apoptosis and also damage skin integrity. Propofol (2,6-diisopropylphenol) has antioxidant properties. In this study, we investigated how propofol influences intracellular autophagy and apoptotic cell death induced by oxidative stress in human keratinocytes. Method: The following groups were used for experimentation: control, cells were incubated under normoxia (5% $CO_2$, 21% $O_2$, and 74% $N_2$) without propofol; hydrogen peroxide ($H_2O_2$), cells were exposed to $H_2O_2$ ($300{\mu}M$) for 2 h; propofol preconditioning (PPC)/$H_2O_2$, cells pretreated with propofol ($100{\mu}M$) for 2 h were exposed to $H_2O_2$; and 3-methyladenine $(3-MA)/PPC/H_2O_2$, cells pretreated with 3-MA (1 mM) for 1 h and propofol were exposed to $H_2O_2$. Cell viability, apoptosis, and migration capability were evaluated. Relation to autophagy was detected by western blot analysis. Results: Cell viability decreased significantly in the $H_2O_2$ group compared to that in the control group and was improved by propofol preconditioning. Propofol preconditioning effectively decreased $H_2O_2$-induced cell apoptosis and increased cell migration. However, pretreatment with 3-MA inhibited the protective effect of propofol on cell apoptosis. Autophagy was activated in the $PPC/H_2O_2$ group compared to that in the $H_2O_2$ group as demonstrated by western blot analysis and autophagosome staining. Conclusion: The results suggest that propofol preconditioning induces an endogenous cellular protective effect in human keratinocytes against oxidative stress through the activation of signaling pathways related to autophagy.

• Journal of The Korean Dental Society of Anesthesiology
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• v.14 no.4
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• pp.213-219
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• 2014

Background: Clinical use of propofol along with remifentanil for intravenous sedation is increasing in these days, but there are not enough researches to evaluate proper target concentration when these drugs are infused by using target controlled infusion (TCI) pump in dental treatment cases. In this study, we compared efficacy of TCI conscious sedation and target concentration of propofol when it used with or without remifentanil during conscious sedation with the help of a TCI for the surgical extraction of impacted teeth. Methods: After IRB approval, all the charts of patients who had undergone surgical extraction of impacted teeth under propofol TCI sedation for 6 months were selected and reviewed for this study. After reviewal of charts, we could divide patients in two groups. In one group (group 1), only propofol was selected for sedation and initial effect site concentration of propofol was $1{\mu}g/ml$ (n = 33), and in another group (group 2), both propofol and remifentanil was infused and initial effect site concentration of each drug was $0.6{\mu}g/ml$ and 1 ng/ml respectively (n = 25). For each group, average propofol target concentration was measured. In addition, we compared heart rate, respiratory rate, and systolic and diastolic blood pressure as well as oxygen saturation. Besides, BIS, sedation scores (OAAS/S), and subjective satisfaction scores were compared. Results: Between group 1 and 2, there were no significant differences in demographics (age, weight and height), and total sedation time. However, total infused dose and the effect site target concentration of propofol was $163.8{\pm}74.5mg$ and $1.13{\pm}0.21{\mu}g/ml$ in group 1, and $104.3{\pm}46.5mg$ and $0.72{\pm}0.26{\mu}g/ml$ in the group 2 with $1.02{\pm}0.21ng/l$ of the effect site target concentration of remifentanil, respectively. During sedation, there were no differences between overall vital sign, BIS and OAAS/S in 2 groups (P > 0.05). However, we figured out patients in group 2 had decreased pain sensation during sedation. Conclusions: Co-administration of propofol along with remifentanil via a TCI for the surgical extraction of impacted teeth may be safe and effective compared to propofol only administration.

• Journal of The Korean Dental Society of Anesthesiology
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• v.14 no.1
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• pp.41-47
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• 2014

Background: Autophagy is a self-eating process that is important for balancing sources of energy at critical times in development and in response stress. Autophagy also plays a protective role in removing clearing damaged intracellular organelles and aggregated proteins as well as eliminating intracellular pathogens. The purpose of the present study was to examine the protective effect of propofol against hypoxic damage using keratinocytes. Methods: Human keratinocytes (HaCaT cells) were obtained from the American Type Culture Collection. Propofol which were made by dissolving them in DMSO were kept frozen at $-4^{\circ}C$ until use. The stock was diluted to their concentration with DMEM when needed. Prior to propofol treatment cells were grown to about 80% confluence and then exposed to propofol at different concentrations (0, 25, 50, 75, $100{\mu}M$) for 2 h pretreatment. Cell viability was measured using a quantitative colorimetric assay with thiazolyl blue tetrazolium bromide (MTT assay), and fluorescence microscopy and western blot analysis were used for evaluation of autophagy processes. Results: The viability of propofol-treated HaCaT cells was increased in a dose-dependent manner. Propofol did not show any significant toxic effect on the HaCaT cells. The autophagy inhibitor, 3-methyladenine, reduced cell viability of hypoxia-injured HaCat cells. Fluorescence microscopy and western blot analysis showed propofol induce autophagy pathway signals. Conclusions: Propofol enhanced viability of hypoxia-injured HaCaT cells and we suggest propofol has cellular protective effects by autophagy signal pathway activation.

• Journal of Veterinary Clinics
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• v.29 no.6
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• pp.447-454
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• 2012

The objective of this study was to determine the effect of propofol and remifentanil combination on hemodynamics and intraocular pressure (IOP), and to compare with those of isoflurane in beagle dogs. Fourteen clinically healthy beagle dogs were divided randomly into 2 groups and each group was consisted with 7 dogs. Anesthetic agents were propofol (0.2 mg/kg/min) plus remifentanil ($0.5{\mu}g/kg/min$, 1% solution in standard saline) in one group (group PRP) and 3% isoflurane in the other group (group ISF). Anesthesia was maintained for 90 min in the both groups. IOP, blood pressure, heart rate and blood gas values (pH, $PaCO_2$, $PaO_2$, $SaO_2$, $tCO_2$, ${HCO_3}^-$) were recorded at 5, 10, 15, 30, 45, 60, 75 and 90 min in the both groups. IOP values in both eyes were significantly decreased in group PRP compared with those in group ISF. but there were no significant differences between two eyes in each group. Systolic, diastolic and mean blood pressures were significantly decreased in group PRP within the normal range. There were no differences between groups in all blood gas parameters. In this study, propofol and remifentanil combination could provide stable IOP and blood pressure compared with isoflurane.

• The Korean Journal of Physiology and Pharmacology
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• v.21 no.6
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• pp.591-598
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• 2017

Propofol is known to cause vasorelaxation of several systemic vascular beds. However, its effect on the pulmonary vasculature remains controversial. In the present study, we investigated the effects of propofol on human pulmonary arteries obtained from patients who had undergone surgery. Arterial rings were mounted in a Multi-Myograph system for measurement of isometric forces. U46619 was used to induce sustained contraction of the intrapulmonary arteries, and propofol was then applied (in increments from $10-300{\mu}m$). Arteries denuded of endothelium, preincubated or not with indomethacin, were used to investigate the effects of propofol on isolated arteries. Propofol exhibited a bifunctional effect on isolated human pulmonary arteries contracted by U46619, evoking constriction at low concentrations ($10-100{\mu}m$) followed by secondary relaxation (at $100-300{\mu}m$). The extent of constriction induced by propofol was higher in an endothelium-denuded group than in an endothelium-intact group. Preincubation with indomethacin abolished constriction and potentiated relaxation. The maximal relaxation was greater in the endothelium-intact than the endothelium-denuded group. Propofol also suppressed $CaCl_2$-induced constriction in the 60 mM $K^+$-containing $Ca^{2+}$-free solution in a dose-dependent manner. Fluorescent imaging of $Ca^{2+}$ using fluo-4 showed that a 10 min incubation with propofol ($10-300{\mu}m$) inhibited the $Ca^{2+}$ influx into human pulmonary arterial smooth muscle cells induced by a 60 mM $K^+$-containing $Ca^{2+}$-free solution. In conclusion, propofol-induced arterial constriction appears to involve prostaglandin production by cyclooxygenase in pulmonary artery smooth muscle cells and the relaxation depends in part on endothelial function, principally on the inhibition of calcium influx through L-type voltage-operated calcium channels.

• Journal of Veterinary Clinics
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• v.16 no.1
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• pp.86-94
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• 1999

To invstigate the available dosage and effects of xylazine as preanesthetics on the propofol anesthesia in the dog, the experimental animals were randomly divided into 3 groups (xylazine 0.55 mg/kg (group 1), 1 mg/kg (group 2) and 2 mg/kg (group 3) were premedicated) and, monitored analgesic and anesthetic effect, body temperature, respiratory rate (breaths/minute), heart rate (beats/minutes). Also, hematological and serum chemical changes were monitored. In all experimental groups, the animals were recumbent just after propofol injection and time difference was not detected. Except vomitting after xylazine injection and insignificant ataxia during recovery, no significant side effects were observed. In group 2, loss of toe-web needle prick response time was slightly longer than group 1 but the response in group 2 and group 3 were similar, In group 2 and 3, the duration of anesthesia was longer than group 1 (2 folds) but there was no difference between group 2 and 3. Recovery time was prolonged in proportion to administration dosage of xylazine. In all experimental groups, the body temperature of animals was decresed gradually according to experimental time but no significant changes were monitored. The heart rate and respiratory rate were significantly (p<0.01, p<0.05) decreased after propofol injection Hematologically, no significant changes were monitored in total leukocye numbers, total erythrocye numbers, MCV, MCH, MCHC, serum GOT and GPT values Significant changes in all groups were not observed except significant increase in BUN, total-protein and abumin values of group 3. On the basis of these result, premedication of xylazine can be helpful in decresing some side effects and the dosage of propofol. 1 mg/kg of xylazine as preanesthetics on the propofol anesthesia in the dog is considered to be available.

• Journal of The Korean Dental Society of Anesthesiology
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• v.2 no.2 s.3
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• pp.97-100
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• 2002

Background: Patient-controlled sedation (PCS) has been blown for a safe and effective sedative method on the same pharmacological concepts of patient-controlled analgesia. Many different kinds of infusion devices have been used but they often have too long nominal infusion rate and lockout time. $Perfuser^{\circledR}$ fm (B. Braun, Germany) is a new PCA device with 999.9 ml/hr nominal infusion rate and minimum 1 min lockout time. In this study, the feasibility of propofol PCS using $Perfuser^{\circledR}$ fm was examined in order to provide a safe satisfactory sedation for dental patients. Methods: Eleven healthy patients presenting for oral surgery were studied. Propofol PCS was performed using $Perfuser^{\circledR}$ fm, which was set to deliver a bolus dose of 5 mg with 999.9 ml/hr nominal infusion rate and 1 min lockout time. Propofol loading dose was randomly assigned to a bolus dose ${\times}$ 0, 2, and 3 (initial bolus). Patients were told to press the bolus button as often as they needed to relieve discomfort. Results: Total infused dose of propofol was mean 1.8 mg/kg/hr and D (Delivery)/A (Attempt) ratio was mean 72.8%. All patients was awake and there were no clinically significant intraoperative side effects during the sedation. Almost all patients were very satisfied with this type of PCS. Conclusion: Propofol PCS using $Perfuser^{\circledR}$ fm infusion pump provided good conscious sedation for dental procedures.

• Journal of the Korean Applied Science and Technology
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• v.35 no.2
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• pp.472-477
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• 2018

The excess molar volumes of a general anesthetics on Purple membrane and Red membrane separated by extraction in Halobacteriun Halobium and in suspensions of vesicle have been determined at $25^{\circ}C$, it was used a excess volume dilatometer. The anesthesia characteristics of general anesthetics, Propofol was fined by our study to correlate with excess molar volume. Excess volume changes of the vesicle measured by excess volume dilatometer, which is an important amino acid and lipid in the purple membrane and red membrane by means of specific weight in Halobacteriun Halobium, were studied by absorption intensity at 280 nm and 330 nm. The particle size analysis and relative turbidity of Purple membrane and Red membrane by means of Propofol were measured for mechanical properties. In the samples where Propofol is incoporated in vesicle, especially, the excess molar volume of PM + RM + Propofol is the greatest than the excess molar volumes of PM, and RM.

• Journal of The Korean Dental Society of Anesthesiology
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• v.10 no.1
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• pp.50-53
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• 2010

There are a few case reports describing persistent seizure following propofol. A 45-year-old female underwent operation of mastoidectomy and tympanoplasty. She had no personal or family history of epilepsy. Anesthesia was induced with propofol and rocuronium, and maintained with sevoflurane-remifentanil after tracheal intubation. Any event was not noted during surgery. Seizure-like movement and shivering were developed after surgery in recovery room. Symptom was relieved by benzodiazepines, especially lorazepam. She was discharged in the 9th postoperative days without any sequelae.