scholarly journals IN-SITU FILM-FORMING SOLUTION FOR TOPICAL APPLICATION OF TERBINAFINE HCL: BIOPHARMACEUTICAL EVALUATION AND IN VIVO ANTIFUNGAL PERFORMANCE USING ANIMAL MODEL

2021 ◽  
pp. 98-105
Author(s):  
MOHD FAIZ MUSTAFFA ◽  
KALAVATHY RAMASAMY ◽  
NAQIBAH JAAFAR ◽  
MIZATON HAZIZUL HASAN ◽  
NOR AMLIZAN RAMLI ◽  
...  
Keyword(s):  
Stratum Corneum ◽  
Topical Application ◽  
Positive Control ◽  
Polyethylene Glycol 400 ◽  
Drug Permeation ◽  
Methacrylate Copolymers ◽  
Film Forming ◽  
Terbinafine Hcl

Objective: The main purpose of this study is to develop a film-forming solution with optimum physical-mechanical characteristics and excellent antifungal activity to enhance deposition and penetration into the stratum corneum (SC). Methods: The film-forming solutions of terbinafine HCl were formulated using methacrylate copolymers, polyethylene glycol 400, and ethanol as diluent. The selected formulations were subjected to test of physical-mechanical properties, drug release, drug permeation across the stratum corneum and drug deposition study. The best formulation was further evaluated for in vivo antifungal efficacy. Results: The selected formulations exhibited superior pharmaceutical characteristics, including rapid drying, non-stickiness, and being transparency on the skin. Formulation A (FA) had significantly lower tensile strength (4.78 N/m2, p<0.05) and higher percentage elongation at break (33.61%, p<0.05), which reduced the firmness of the film, allowing it to be super-flexible in following the movement of the skin and preventing loss of film through abrasion. FA showed significantly (p<0.05) rapid drug permeation (1510.51 µg/cm2) across the stratum corneum (SC) at 24 h when compared with the other formulations and the positive control proprietary drug (PD), Terbex® cream formulation (475.8 µg/cm2). Conclusion: Having superior physical-mechanical and drug permeation characteristics, FA can be considered as an efficient, reproducible, and efficacious antifungal formulation for topical application.

scholarly journals Quantification method for timolol from in vivo samples for the development of a new glaucoma drug depot

2018 ◽  
Vol 4 (1) ◽  
pp. 225-227
Author(s):  
Thomas Eickner ◽  
Franziska Kopp ◽  
Andreas Brietzke ◽  
Sabine Kischkel ◽  
Stefan Oschatz ◽  
...  
Keyword(s):  
Drug Release ◽  
Topical Application ◽  
Aqueous Humour ◽  
Liquid Chromatography Mass Spectrometry ◽  
Timolol Maleate ◽  
Sustained Drug Release ◽  
Subconjunctival Space ◽  
New Zealand White Rabbits

AbstractGlaucoma is the second most common cause of blindness. An increased intraocular pressure is the only treatable symptom of glaucoma. Because patients often exhibit a poor therapy adherence, a drug depot consisting of ELA-NCO and hyaluronic acid with timolol was developed to ensure sustained drug release. This drug depot is formed by in situ polymerisation after injection into the subconjunctival space. To test the in vivo drug release of timolol in serum and aqueous humour, a liquid chromatography mass spectrometry (LCMS) method was developed and tested using spike- and recovery experiments, and on in vivo samples after topical application. Samples of serum and aqueous humour were taken from New Zealand White rabbits. For topical application, a commercially available formulation of timolol was used. This study presents results concerning the recovery of timolol from spiked samples. Serum and aqueous humour samples were spiked with timolol maleate to a final concentration of 50 ng/mL. Subsequently, the samples were extracted and analysed by LCMS. External calibration of the developed method showed high linearity. Recovery experiments showed no loss of timolol. Hence, the extraction method is robust and able to recover the whole amount of timolol from aqueous humour and serum.

Formulation and evaluation of resveratrol loaded cubosomal nanoformulation for topical delivery

2020 ◽  
Vol 17 ◽  
Author(s):  
Bhaskar Kurangi ◽  
Sunil Jalalpure ◽  
Satveer Jagwani
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Topical Application ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Drug Permeation

Aim: The aim of the study was to formulate, characterize, and evaluate the resveratrol-loaded cubosomes (RC) through topical application. Background: Resveratrol (RV) is a nutraceutical compound that has exciting pharmacological potential in different diseases including cancers. Many studies of resveratrol have been reported for anti-melanoma activity. Due to its low bioavailability, the activities of resveratrol are strongly limited. Hence, an approach with nanotechnology has been done to increase its activity through transdermal drug delivery. Objective: To formulate, characterize, and evaluate the resveratrol-loaded cubosomes (RC). To evaluate resveratrol-loaded cubosomal gel (RC-Gel) for its topical application. Methods: RC was formulated by homogenization technique and optimized using a 2-factor 3-level factorial design. Formulated RCs were characterized for particle size, zeta potential, and entrapment efficiency. Optimized RC was evaluated for in vitro release and stability study. Optimized RC was further formulated into cubosomal gel (RC-Gel) using carbopol and evaluated for drug permeation and deposition. Furthermore, developed RC-Gel was evaluated for its topical application using skin irritancy, toxicity, and in vivo local bioavailability studies. Results: The optimized RC indicated cubic-shaped structure with mean particle size, entrapment efficiency, and zeta potential were 113±2.36 nm, 85.07 ± 0.91%, and -27.40 ± 1.40 mV respectively. In vitro drug release of optimized RC demonstrated biphasic drug release with the diffusion-controlled release of resveratrol (RV) (87.20 ± 2.25%). The RC-Gel demonstrated better drug permeation and deposition in mice skin layers. The composition of RC-Gel has been proved non-irritant to the mice skin. In vivo local bioavailability study depicted the good potential of RC-Gel for skin localization. Conclusion: The RC nanoformulation proposes a promising drug delivery system for melanoma treatment simply through topical application.

scholarly journals In Vitro Evaluation of Poly(lactide-co-glycolide) In Situ Forming Gels for Bedaquiline Fumarate Salt and Pharmacokinetics Following Subcutaneous Injection in Rats

Pharmaceutics ◽  
2021 ◽  
Vol 13 (8) ◽  
pp. 1231
Author(s):  
Sandy Van Hemelryck ◽  
Rani Wens ◽  
Hannelore van Poppel ◽  
Milou Luijks ◽  
Koosha Shahidi ◽  
...  
Keyword(s):  
Drug Release ◽  
Point Of View ◽  
Solvent Ratio ◽  
Sustained Drug Release ◽  
Polyethylene Glycol 400 ◽  
In Situ Forming ◽  
Fumarate Salt

This study evaluated in vitro and in vivo drug release of bedaquiline from in situ forming gels (ISGs) containing 200 mg eq./g bedaquiline fumarate salt prepared with four different grades of poly(d,l-lactide) (PDLLA) or poly(d,l-lactide-co-glycolide) (PLGA) with a lactide/glycolide ratio of 50/50 or 75/25 and acid (A) or ester (E) end-capping in N-methyl-2-pyrrolidone at a polymer/solvent ratio of 20/80% (w/w). Mean in vitro drug release in 0.05 M phosphate buffer pH 7.4 with 1% (w/v) sodium lauryl sulphate was 37.3, 47.1, 53.3, and 62.3% within 28 days for ISGs containing PLGA5050A, PDLLA, PLGA7525A, and PLGA7525E, respectively. The data suggested that drug release was primarily controlled by precipitated drug redissolving, rather than polymer erosion. In vivo pharmacokinetic profiles after subcutaneous injections in rats were comparable for all ISGs (mean half-lives (t1/2) ranged from 1411 to 1695 h) and indicated a sustained drug release when compared to a solution of bedaquiline fumarate salt in polyethylene glycol 400/water 50/50% (v/v) (mean t1/2 of 895 h). In conclusion, PLGA or PDLLA-based ISGs have shown potential for parenteral sustained delivery of bedaquiline, suggesting further preclinical and clinical studies. From a formulation point of view, this case example highlights the importance of the interplay between drug solubility in biological media and dissolution of drug precipitates, which, in addition to the incorporation of diffusion controlling polymers, governs the release of the active drug.

Potentiation of Bradykinin by Angiotensin-(1-7) on Resistance Vessels of Hypertensive Rats, Studied in Vivo .

Hypertension ◽  
2000 ◽  
Vol 36 (suppl_1) ◽  
pp. 696-696
Author(s):  
Liliam Fernandes ◽  
Zuleica B Fortes ◽  
Dorothy Nigro ◽  
Regina Scivoletto ◽  
Robson A S Santos ◽  
...  
Keyword(s):  
Topical Application ◽  
Ace Inhibition ◽  
Pharmacological Effects ◽  
Hypertensive Rats ◽  
Specific Receptor ◽  
Resistance Vessels ◽  
Before And After ◽  
Arteriolar Diameter

P19 Objective: To verify the Angiotensin-(1-7) [Ang-(1-7)]-activity on Bradykinin (BK)-induced vasodilation in SHR mesenteric arterioles, in vivo-in situ. Methods: Arteriolar diameter was measured by intravital microscopy before and after topical application of BK(1pmol), Acetylcholine(ACh 1.6nmol), Sodium nitroprusside (SNP 38pmol) or Histamine (5.4nmol) in the absence or presence of Ang-(1-7) (100pmol). To investigate the Ang-(1-7)/BK interaction, treatments were employed through topical application of antagonists of BK (HOE140,100pmol), Ang-(1-7)(A779,100pmol)and potassium channel (tetraethylammoniun - TEA,90pmol), with an inhibitor of NOSynthase (L-NAME 10nmol) and after cyclooxygenase blockade (indomethacin 5mg/Kg or diclofenac 2.5mg/Kg). To evaluate the effect of ACE- and/or AT 1 blockade on Ang-(1-7)/BK interaction, rats were treated for 21 days with enalapril, quinapril (10mg/Kg), losartan (15mg/Kg) or enalapril + losartan (10 and 15 mg/Kg, respectively). In those enalapril-treated rats the effect of BK (1pmol) was also analysed in the presence of A779 (100pmol). Results: BK-induced vasodilation, but not ACh, SNP or Histamine responses, was increased in the presence of Ang-(1-7) (4.96±0.7% vs 9.07±1.0% * ).This interaction was abolished by HOE (1.11±0.8% * ), A779 (5.13±0.6% * ), TEA (3.37±0.5% * ), indomethacin (1.73±0.4% * )and diclofenac (3.63±0.5% * ), whereas L-NAME did not modify the Ang-(1-7)-potentiating activity. The BK-potentiation by Ang-(1-7) was also observed after enalapril (10.57±0.5% * ), quinapril (8.9±0.7% * ), losartan (9.93±1.2% * ) and enalapril + losartan (10.59±0.5% * ). Enalapril increased the BK-vasodilation(8.21±0.7% * ), but this effect was reversed in the presence of A779 (4.27±0.5% * ). * p≤0.05 Conclusion: In the SHR microcirculation Ang-(1-7) potentiates BK through a specific receptor, probably releasing prostaglandins and EDHF. Our results indicate that the BK-potentiation by Ang-(1-7) may occur endogenously and contribute to the pharmacological effects of ACE inhibition. HOE 140 and Quinapril were gifts from HOECHST and Warner Lambert, respectively.

scholarly journals EFFICACY OF A STANDARDIZED ETHANOL EXTRACT OF ROSELLE CALYX IN THE TREATMENT OF ORAL MUCOSA ULCERATION (IN VIVO)

2017 ◽  
Vol 10 (17) ◽  
pp. 183
Author(s):  
Reni Jayantini ◽  
Dewi Fatma Suniarti ◽  
Agoeng T Sarwono
Keyword(s):  
Topical Application ◽  
Ethanol Extract ◽  
Negative Control Group ◽  
Positive Control ◽  
Negative Control ◽  
Control Group ◽  
Sprague Dawley ◽  
Ethanol Extracts ◽  
Inflammation Score

 Objectives: To analyze the effectiveness of the topical application of a standardized ethanol extract of roselle calyx in the treatment of oral mucous ulceration.Methods: Twelve Sprague Dawley rats were divided into two groups, with oral mucous ulcer being induced in all the rats. The ulcer diameter, reddish color, and the swollen membrane around the ulcer, as well as the inflammation score of the ulcer, were recorded for all animals. The negative control group was treated with aquades, while the positive control group was treated with 0.1% triamcinolone acetonide. The treatment group received the topical application of 7.5% and 15% standardized ethanol extract of roselle calyx twice a day for 3 or 7 days. On the 4th day, six rats were sacrificed, while the remaining six rats continued to receive treatment as before. On the 8th day, all the rats were sacrificed. Specimens were fixed, and histology slides were made. Further, microscopic slides were observed and scored.Result: Both the 7.5% and 15% standardized ethanol extracts of roselle calyx were found to reduce the ulcer diameter and inflammation score. No swelling or redness was observed.Conclusions: The application of 7.5% standardized ethanol extract of roselle calyx for 7 days is equally as effective as the application of 0.1% triamcinolone acetonides, except in terms of the decrease in the inflammation score.

scholarly journals IN SITU EXPERIMENT FOR EVALUATING IN VIVO CUTANEOUS PHARMACOKINETICS OF FLURBIPROFEN AFTER TOPICAL APPLICATION

1997 ◽  
Vol 12 (supplement) ◽  
pp. 98-99
Author(s):  
Go YANAGIMOTO ◽  
Teruaki HAYASHI ◽  
Toshinobu SEKI ◽  
Kazuhiko JUNI ◽  
Kenji SUGIBAYASHI ◽  
...  
Keyword(s):  
Topical Application ◽  
In Situ Experiment

scholarly journals DESIGNING OF NOVEL TOPICAL IN SITU POLYMERIC FILM-FORMING SOLUTION SPRAY FORMULATION OF ANTIFUNGAL AGENT: IN VITRO ACTIVITY AND IN VIVO CHARACTERIZATION

2022 ◽  
pp. 169-184
Author(s):  
NABIL ABDULLAH ◽  
AMIT B. PATIL
Keyword(s):  
Ex Vivo ◽  
Skin Irritation ◽  
Inhibition Zone ◽  
Wistar Rat ◽  
Polymeric Film ◽  
Film Forming ◽  
Spray Formulation

Objective: Voriconazole (VCZ) is a broad-spectrum antifungal medication that works by inhibiting fungal Cytochrome P450, preventing fungi growth. The current study aims at developing and characterizing an antifungal in situ film-forming polymeric solution spray containing VCZ for use in topical drug delivery systems. Methods: Optimized VCZ in situ polymeric film formulation was evaluated for Fourier transform infrared spectroscopy (FTIR), differential scanning calorimeter (DSC), X-ray diffractometry (XRD), Scanning electron microscope (SEM), in vitro and in vivo, ex-vivo investigation using abdominal rat skin and stability studies. The in vivo antifungal activity of the advanced in situ film was examined in albino Wistar rats. Results: The optimized batch contained 22% Eudragit RS 100 (ERS) and 4% Sorbitol. Based on FTIR, XRD, SEM, and rheological studies. Formulation ingredients of VCZ loaded topical in situ polymeric film spray were observed to be compatible and showed no evidence of precipitation, deformation, or discoloration. Diffusion test (in vitro %), and ex-vivo drug diffusion % obtained 99.22%, and 97.45% respectively. The maximum inhibition zone was measured at 13±0.07 mm. The Wistar rat was employed as an animal model for skin irritation and antifungal studies. A study of short-term stability observed no significant modifications in the physical properties. Conclusion: The findings of the optimized VCZ topical in situ polymeric film spray formulation were satisfactory, demonstrating comparable improvement in superficial antifungal treatment.

Gastric and duodenal HCO3- transport in vivo: influence of prostaglandins

1983 ◽  
Vol 245 (6) ◽  
pp. G751-G759 ◽  
Author(s):  
L. A. Smeaton ◽  
B. H. Hirst ◽  
A. Allen ◽  
A. Garner
Keyword(s):  
Prostaglandin E2 ◽  
Surface Area ◽  
Topical Application ◽  
Mammalian Species ◽  
Electrical Potential ◽  
Duodenal Mucosa ◽  
Electrical Potential Difference ◽  
Ph Stat

Gastric and duodenal HCO3- transport was compared in the same mammalian species (cat) in vivo. The most appropriate technique for detecting HCO3- in the lumen of the stomach was measurement of pH and CO2 tension, whereas in the duodenum it was pH-stat titration. For experiments on gastric HCO3- transport, conscious cats prepared with vagally denervated fundic pouches were used; for those on duodenal transport anesthetized animals with in situ perfused segments were studied. When expressed in terms of gross surface area, basal HCO3- output was six times greater in the duodenum than in the stomach (approximately 1.5 cf. approximately 0.25 mumol X cm-2 X 15 min-1). topical application of 16,16-dimethyl prostaglandin E2 (dmPGE2) to duodenal mucosa caused a concentration-dependent increase in HCO3- output and transmucosal electrical potential difference (PD) over the range 0.01–1.0 microgram X ml-1. PGE2 was approximately 200 times less potent than dmPGE2 as a stimulant of duodenal HCO3- transport. Increases in the rate of luminal HCO3- output following application of dmPGE2 were considerably less in the stomach compared with the duodenum (approximately 50% cf. approximately 1,000% at 1 microgram X ml-1). Intravenous dmPGE2 (1 microgram X kg-1 X h-1) had no effect on either gastric or duodenal HCO3- outputs. Indomethacin (5 mg X kg-1 iv) inhibited duodenal HCO3- output by approximately 50% and reduced PD but did not influence gastric HCO3- output. We propose that in the cat duodenum in vivo local prostaglandins regulate HCO3- transport, but in the cat stomach in vivo they have a less important role.

In vitro and in vivo polysaccharides assembly: ultrastructural and cytochemical study of growing plant cell wall components.

1978 ◽  
Vol 36 (2) ◽  
pp. 434-435
Author(s):  
D. Reis ◽  
B. Vian ◽  
J. C. Roland
Keyword(s):  
Cell Wall ◽  
Self Assembly ◽  
Plant Cell Wall ◽  
Higher Plants ◽  
Three Dimensional ◽  
Cytochemical Study ◽  
Wall Components

Wall morphogenesis in higher plants is a problem still open to controversy. Until now the possibility of a transmembrane control and the involvement of microtubules were mostly envisaged. Self-assembly processes have been observed in the case of walls of Chlamydomonas and bacteria. Spontaneous gelling interactions between xanthan and galactomannan from Ceratonia have been analyzed very recently. The present work provides indications that some processes of spontaneous aggregation could occur in higher plants during the formation and expansion of cell wall.Observations were performed on hypocotyl of mung bean (Phaseolus aureus) for which growth characteristics and wall composition have been previously defined.In situ, the walls of actively growing cells (primary walls) show an ordered three-dimensional organization (fig. 1). The wall is typically polylamellate with multifibrillar layers alternately transverse and longitudinal. Between these layers intermediate strata exist in which the orientation of microfibrils progressively rotates. Thus a progressive change in the morphogenetic activity occurs.

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