scholarly journals Effect of two surfactants on in vitro permeation of butorphanol through horse nasal mucosa

Uniciencia ◽  
2021 ◽  
Vol 35 (2) ◽  
pp. 1-10
Author(s):  
María Inés Velloso ◽  
Héctor Alfredo Andreeta ◽  
María Fabiana Landoni
Keyword(s):  
Nasal Mucosa ◽  
Tween 80 ◽  
Ionic Surfactant ◽  
Apparent Permeability ◽  
In Vitro Permeation ◽  
Apparent Permeability Coefficient ◽  
Dose Control ◽  
Franz Diffusion Cells ◽  
Cetrimonium Bromide

The aim of the present study was to evaluate the effect of two surfactants on in vitro permeation of butorphanol through equine nasal mucosa. Franz diffusion cells and equine nasal mucosa were used. Three formulations were developed based on citric acid, sodium citrate, sodium chloride, and butorphanol tartrate and administered at a 24.4 g cm-3 dose. Control formulation lacked any penetration enhancer. Formulation 1 (F1) had a cationic surfactant (cetrimonium bromide) and formulation 2 (F2) had a non-ionic surfactant (Tween 80). Statistically comparing flux values at the steady state (Jss), apparent permeability coefficient (Kp), and lag-time from control, F1 and F2 for the respiratory region does not show statistically significant differences (α= 0.05). However, statistically significant differences were found on the Jss and Kp, values from control, F1, and F2 in olfactory mucosa. A statistical analysis on the latter showed significant differences between the Jss values of F1 and F2 and between control and F2. Based on this, Tween 80 proved to be a promising excipient in developing intranasal butorphanol formulations in equines since it increases its passage through the nasal mucosa. These results are very promising to continue with the development of intranasal butorphanol formulation in equines.

scholarly journals EFECTO DE UN SURFACTANTE NO IONICO EN LA PERMEABILIDAD DE BUTORFANOL A TRAVES DE MUCOSA NASAL EQUINA

2021 ◽  
Vol 19 (suplemento) ◽  
Author(s):  
M I Velloso
Keyword(s):  
Intranasal Administration ◽  
Tween 80 ◽  
Ionic Surfactant ◽  
Apparent Permeability ◽  
In Vitro Permeation ◽  
Equine Medicine ◽  
Site Of Action ◽  
The Central Nervous System ◽  
Franz Diffusion Cells

Implementation of intranasal administration for the delivery of drugs with site of action into the central nervous system, such as butorphanol, became a potential choice in equine medicine.  In this study, using Franz-diffusion cells the in vitro permeation rate through respiratory and olfactory equine nasal mucosa of two butorphanol formulations was estimated and compared.  Both formulations had the same composition, was the exception for formulation 2, that contained 2, 5 x 10 -4 M of a non-ionic surfactant (tween 80). Butorphanol administered dose was 24, 4 mg/cm2. Plots of the cumulative amounts of butorphanol against time were constructed, where maximum flux values at the steady state (Jss), apparent permeability coefficients (Kp) and lag-time (tlag) were estimated. The Jss and Kp show that permeation of butorphanol through olfactory mucosa is different than respiratory mucosa. Moreover, Jss for formulation 2 was higher than formulation 1 in both anatomical areas, probably for the effect of the surfactant. The present results are promising to carry on with the development of formulation of butorphanol for intranasal administration.

scholarly journals Validation of an Ex Vivo Permeation Method for the Intestinal Permeability of Different BCS Drugs and Its Correlation with Caco-2 In Vitro Experiments

Pharmaceutics ◽  
2019 ◽  
Vol 11 (12) ◽  
pp. 638 ◽  
Author(s):  
Aroha B. Sánchez ◽  
Ana C. Calpena ◽  
Mireia Mallandrich ◽  
Beatriz Clares
Keyword(s):  
Ex Vivo ◽  
Colon Adenocarcinoma ◽  
Apparent Permeability ◽  
Pharmaceutical Dosage Forms ◽  
Diffusion Cells ◽  
Intestinal Membrane ◽  
Ex Vivo Permeation ◽  
Apparent Permeability Coefficient ◽  
Franz Diffusion Cells

The absorption study of drugs through different biological membranes constitutes an essential step in the development of new pharmaceutical dosage forms. Concerning orally administered forms, methods based on monolayer cell culture of Caco-2 (Caucasian colon adenocarcinoma) have been developed to emulate intestinal mucosa in permeability studies. Although it is widely accepted, it has disadvantages, such as high costs or high technical complexity, and limitations related to the simplified structure of the monolayer or the class of molecules that can be permeated according to the transport mechanisms. The aim of this work was to develop a new ex vivo methodology which allows the evaluation of the intestinal apparent permeability coefficient (Papp) while using fewer resources and to assess the correlation with Caco-2. To this end, pig (Sus scrofa) duodenum segments were mounted in Franz diffusion cells and used to permeate four different drugs: ketorolac tromethamine (Kt), melatonin (Mel), hydrochlorothiazide (Htz), and furosemide (Fur). No statistically significant differences (p > 0.05) were observed corelating Papp values from Franz diffusion cells and Caco-2 cell experiments for Kt, Htz, and Fur. However, there were statistically significant differences (p < 0.05) correlating Papp values and Mel. The difference is explained by the role of Mel in the duodenal epithelial paracellular permeability reduction. Ex vivo permeation may be an equivalent method to Caco-2 for drugs that do not produce intestinal membrane phenomena that could affect absorption.

Bicarbonate secretion in rat distal colon in vitro: a measurement technique

1988 ◽  
Vol 254 (3) ◽  
pp. C383-C390 ◽  
Author(s):  
G. M. Feldman ◽  
S. F. Berman ◽  
R. L. Stephenson
Keyword(s):  
Short Circuit ◽  
Distal Colon ◽  
Apparent Permeability ◽  
Chemical Gradients ◽  
Acid Generation ◽  
Rat Distal Colon ◽  
Tissue Surfaces ◽  
Apparent Permeability Coefficient ◽  
Transepithelial Voltage

To study HCO3- secretion in rat distal colon, we utilized a technique that permits control of electrical and chemical transepithelial gradients. With symmetrical solutions (pH 7.4, [HCO3-] 25 mM, and CO2 tension 40 mmHg) bathing both tissue surfaces and under short-circuit conditions, HCO3- secretion remained stable for greater than 4 h at 1 mueq. h-1.cm-2. As the mucosal solution was alkalinized, the serosal solution was acidified at 3.1 mueq.h-1.cm-2. Ninety-four percent of serosal acidification was accounted for by the rate of metabolic lactic acid generation and transepithelial HCO3- secretion. Clamping transepithelial voltage reversibly affected net HCO3- secretion, and a linear relationship existed between clamped mucosal voltage and net HCO3- flux (r = 0.99); mucosal voltage of -68 mV completely inhibited net secretion. The apparent permeability coefficient of the colon to HCO3- is 2.8 X 10(-6) cm/s. One millimolar ouabain completely inhibited net HCO3- secretion. Acetazolamide (10(-4) M) inhibited secretion by approximately 50%, whereas a 10(-3) M concentration inhibited secretion by 90%. These data demonstrate that net colonic HCO3- secretion can be measured without imposed electrical and chemical gradients and that this flux is voltage sensitive and depends on carbonic anhydrase and Na+-K+-ATPase activities.

Development and evaluation of a heparin gel for transdermal delivery via laser-generated micropores

2021 ◽  
Vol 12 (2) ◽  
pp. 133-144
Author(s):  
Deepal Vora ◽  
Yujin Kim ◽  
Ajay K Banga
Keyword(s):  
Transdermal Delivery ◽  
Continuous Intravenous Infusion ◽  
In Vitro Permeation ◽  
Assisted Delivery ◽  
Permeation Studies ◽  
Franz Diffusion Cells ◽  
Transdermal Route ◽  
Poloxamer Gel ◽  
Ablative Laser

Aim: Our study investigated the feasibility of transdermal delivery of heparin, an anticoagulant used against venous thromboembolism, as an alternative to intravenous administration. Materials & methods: Skin was pretreated using ablative laser (Precise Laser Epidermal System [P.L.E.A.S.E.®] technology) for enhanced delivery of heparin. In vitro permeation studies using static Franz diffusion cells provided a comparison between delivery from 0.3% w/v heparin-loaded poloxamer gel and solution across untreated and laser-treated dermatomed porcine ear skin. Results: No passive delivery of heparin was observed. Laser-assisted delivery from solution (26.07 ± 1.82 μg/cm2) was higher (p < 0.05) than delivery from heparin gel (11.28 ± 5.32 μg/cm2). However, gel is likely to sustain the delivery over prolonged periods like a maintenance dose via continuous intravenous infusion. Conclusion: Thus, ablative laser pretreatment successfully delivered heparin, establishing the feasibility of delivering hydrophilic macromolecules using the transdermal route.

scholarly journals Effect of Topical Liposomes Containing Paromomycin Sulfate in the Course of Leishmania major Infection in Susceptible BALB/c Mice

2009 ◽  
Vol 53 (6) ◽  
pp. 2259-2265 ◽  
Author(s):  
Mahmoud R. Jaafari ◽  
Neda Bavarsad ◽  
Bibi Sedigheh Fazly Bazzaz ◽  
Afshin Samiei ◽  
Dina Soroush ◽  
...  
Keyword(s):  
Leishmania Major ◽  
Mouse Skin ◽  
Parasite Burden ◽  
Lesion Size ◽  
Control Group ◽  
In Vitro Permeation ◽  
Significant Difference ◽  
Pm 10 ◽  
Franz Diffusion Cells

ABSTRACT The aim of this study was to evaluate the antileishmanial effects of topical liposomal paromomycin sulfate (PM) in Leishmania major-infected BALB/c mice. Liposomes containing 10 or 15% PM (Lip-PM-10 and Lip-PM-15, respectively) were prepared by the fusion method and were characterized for their size and encapsulation efficiency. The penetration of PM from the liposomal PM formulations (LPMFs) through and into skin was evaluated in vitro with Franz diffusion cells fitted with mouse skin at 37°C for 8 h. The in vitro permeation data showed that almost 15% of the LPMFs applied penetrated the mouse skin, and the amount retained in the skin was about 60% for both formulations. The 50% effective doses of Lip-PM-10 and Lip-PM-15 against L. major promastigotes in culture were 65.32 and 59.73 μg/ml, respectively, and those against L. major amastigotes in macrophages were 24.64 and 26.44 μg/ml, respectively. Lip-PM-10 or Lip-PM-15 was used topically twice a day for 4 weeks to treat L. major lesions on BALB/c mice, and the results showed a significantly (P < 0.001) smaller lesion size in the mice in the treated groups than in the mice in the control group, which received either empty liposomes or phosphate-buffered saline (PBS). Eight weeks after the beginning of the treatment, every mouse treated with LPMFs was completely cured. The spleen parasite burden was significantly (P < 0.001) lower in mice treated with Lip-PM-10 or Lip-PM-15 than in mice treated with PBS or control liposomes, but no significant difference was seen between the two groups treated with either Lip-PM-10 or Lip-PM-15. The results suggest that topical liposomal PM may be useful for the treatment of cutaneous leishmaniasis.

scholarly journals Development and In Vitro Evaluation of a Mucoadhesive Oral Deliverv System for Antisense Oliaonucleotides

2003 ◽  
Vol 71 (3) ◽  
pp. 165-177 ◽  
Author(s):  
Andreas Bernkop-Schnürch ◽  
Julia Telsnig ◽  
Margit Hornof
Keyword(s):  
Delivery System ◽  
Permeability Coefficient ◽  
Enzymatic Degradation ◽  
Phosphorothioate Oligonucleotide ◽  
Apparent Permeability ◽  
Release Studies ◽  
Apparent Permeability Coefficient ◽  
Permeation Studies ◽  
Membrane Bound

It was the aim of this study to develop an oral phosphorothioate oligodeoxynucleotide (PS-ODN) drug delivery system and to evaluate its properties in vitro. Results demonstrated that the 16-mer phosphorothioate oligonucleotide used was completely stable towards enzymatic degradation by secreted and membrane bound intestinal enzymes. Permeation studies with freshly excised intestinal mucosa showed a comparatively high uptake of the PS-ODN with an apparent permeability coefficient (Papp) of 8.35 ± 1.24 x 10-6 cm/sec. The PS-ODN was incorporated in a poly(acrylic acid)-cysteine carrier matrix system exhibiting high cohesive and mucoadhesive properties. Release studies demonstrated that a controlled and sustained PS-ODN release out of this delivery system could be achieved. Because of these features, the dosage form developed within this study seems to represent a promising novel tool for oral PS-ODN delivery.

scholarly journals Transport of Corilagin, Gallic Acid, and Ellagic Acid from Fructus Phyllanthi Tannin Fraction in Caco-2 Cell Monolayers

2016 ◽  
Vol 2016 ◽  
pp. 1-10 ◽  
Author(s):  
Xin Mao ◽  
Ling-Fang Wu ◽  
Hai-juan Zhao ◽  
Wen-Yi Liang ◽  
Wen-Jing Chen ◽  
...  
Keyword(s):  
Tight Junction ◽  
Gallic Acid ◽  
Ellagic Acid ◽  
Organic Anion ◽  
Multidrug Resistance Proteins ◽  
Apparent Permeability ◽  
Glycoprotein P ◽  
Sodium Glucose Cotransporter ◽  
Apparent Permeability Coefficient

Objective. To investigate the absorption property of the representative hydrolyzable tannin, namely corilagin, and its hydrolysates gallic acid (GA) and ellagic acid (EA) from the Fructus Phyllanthi tannin fraction (PTF)in vitro.Methods. Caco-2 cells monolayer model was established. Influences of PTF on Caco-2 cells viability were detected with MTT assay. The transport across monolayers was examined for different time points, concentrations, and secretory directions. The inhibitors of P-glycoprotein (P-gp), multidrug resistance proteins (MRPs), organic anion transporting polypeptide (OATP) and sodium/glucose cotransporter 1 (SGLT1), and tight junction modulators were used to study the transport mechanism. LC-MS method was employed to quantify the absorption concentration.Results. The apparent permeability coefficient(Papp)values of the three compounds were below 1.0 × 10−6 cm/s. The absorption of corilagin and GA were much lower than their efflux, and the uptake of both compounds was increased in the presence of inhibitors of P-gp and MRPs. The absorption of EA was decreased in the company of OATP and SGLT1 inhibitors. Moreover, the transport of corilagin, GA, and EA was enhanced by tight junction modulators.Conclusion. These observations indicated that the three compounds in PTF were transported via passive diffusion combined with protein mediated transport. P-gp and MRPs might get involved in the transport of corilagin and GA. The absorption of EA could be attributed to OATP and SGLT1 protein.

In vitro permeation of several model drugs across rabbit nasal mucosa

1994 ◽  
Vol 103 (1) ◽  
pp. 27-36 ◽  
Author(s):  
Hiroyuki Kubo ◽  
Ken-Ichi Hosoya ◽  
Hideshi Natsume ◽  
Kenji Sugibayashi ◽  
Yasunori Morimoto
Keyword(s):  
Nasal Mucosa ◽  
In Vitro Permeation

scholarly journals PREPARATION AND IN VITRO EVALUATION OF FAST RELEASE DIAZEPAM SUPPOSITORIES FOR FEBRILE SEIZURES

2017 ◽  
Vol 10 (9) ◽  
pp. 365
Author(s):  
Aseel Alsamman ◽  
Mohammad Othman
Keyword(s):  
Tween 80 ◽  
Febrile Seizures ◽  
Water Soluble ◽  
Infrared Spectrometry ◽  
Ionic Surfactant ◽  
Scanning Calorimetry ◽  
Water Soluble Polymer ◽  
In Vitro Drug Release ◽  
Fast Release

  Objective: The objective of this study was to optimize the best formula for fast release suppositories of diazepam.Methods: Suppositories were prepared by fusion method using Witepsol H15 as oleaginous base, polyethylene glycol as a water-soluble polymer, and Poloxamer 188 as water miscible base. All suppositories were evaluated for physical characteristics, in vitro drug release and kinetic models. The effects of incorporating Tween 80 as a non-ionic surfactant, propylene glycol as a cosolvent, and effervescent pair on the release rate of diazepam from suppositories were investigated. Differential scanning calorimetry and Fourier transform infrared spectrometry were used to characterize physical mixtures of diazepam and the different used bases.Results: Many formulations of diazepam have been prepared and in vitro evaluated. PEG suppositories released diazepam more efficiently than poloxamer and witepsol suppositories. The including of an effervescent pair in the formulation of suppositories greatly enhanced the release of diazepam. The addition of tween 80 to witepsol suppositories, PG to poloxamer suppositories, increased the rate and extent of diazepam release.Conclusion: Fast release of diazepam has been obtained from suppositories containing the effervescent pair (formula F3), which also have good physical properties.

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