Enhanced Permeation of Antiemetic Drug from Buccoadhesive Tablets by Using Bile Salts as Permeation Enhancers: Formulation characterization, In Vitro and Ex Vivo Studies

The purpose of this research was to prepare and evaluate monolithic drug-in-adhesive type patches of Rasagiline Mesylate (RM) containing penetration enhancer and having seven day wear property. Preformulation studies like solubility in permeation enhancers, compatibility study, transmission study, uptake study and crystallization study of Rasagiline Mesylate in various pressure sensitive adhesive polymers were performed. Transdermal system was prepared by solvent casting method. The effects of various permeation enhancers (Propylene Glycol, Oleic Acid, Isopropyl Palmitate, and lauryl lactate) on the ex-vivo transcutaneous absorption of Rasagiline Mesylate through human cadaver skin were evaluated by modified Franz diffusion cell system. Ex-vivo transcutaneous absorption of prepared transdermal patch was performed using different concentration of Lauryl lactate (3%, 5%, and 7%). In-vitro Adhesion testing (Peel, tack shear etc.) was performed on different dry GSM (Grams per Square Meter) of patch like 80GSM, 100 GSM and 150 GSM. The final transdermal patches were tested for appearance, weight of matrix, thickness, % assay of drug content, in-vitro adhesion testing, cold flow study and ex-vivo skin permeation studies. Based on crystallization study and adhesion testing, Durotak-4098 (14% drug concentration) was selected as pressure sensitive adhesive. Patch containing Lauryl lactate showed highest cumulative permeation compared to other permeation enhancers. The patch containing 5% laurel lactate showed greater transdermal flux (2.36 µg/cm2 /hr). Patch with 150 dry GSM showing promising adhesion properties. Backing film Scotchpak 9723 and release liner Saint Gobain 8310 was selected based on transmission and uptake study of Rasagiline Mesylate. Stability study indicates that developed formulation remains stable. In conclusion, the present research confirms the practicability of developing Rasagiline Mesylate transdermal system.

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Mucoadhesive microspheres for nasal administration of an antiemetic drug, metoclopramide: in-vitro/ex-vivo studies

Journal of Pharmacy and Pharmacology ◽

10.1211/0022357055623 ◽

2005 ◽

Vol 57 (3) ◽

pp. 287-294 ◽

Cited By ~ 74

Author(s):

Elisabetta Gavini ◽

Giovanna Rassu ◽

Vanna Sanna ◽

Massimo Cossu ◽

Paolo Giunchedi

Keyword(s):

Ex Vivo ◽

Nasal Administration ◽

Antiemetic Drug

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Microemulsions as Solubilizers and Penetration Enhancers for Minoxidil Release from Gels

Gels ◽

10.3390/gels7010026 ◽

2021 ◽

Vol 7 (1) ◽

pp. 26

Author(s):

Miroslava Špaglová ◽

Mária Čuchorová ◽

Martina Čierna ◽

Silvester Poništ ◽

Katarína Bauerová

Keyword(s):

Drug Release ◽

Ex Vivo ◽

Penetration Enhancers ◽

Permeation Enhancers ◽

Permeable Membrane ◽

Ex Vivo Permeation ◽

Residual Amount ◽

Natural Surfactants

Micro- and nanoemulsions are potential drug solubilizers and penetration enhancers through the high surfactant/co-surfactant content. This study aimed to evaluate the influence of minoxidil (MXD) solubilized in the microemulsions (MEs) on drug release by in vitro/ex vivo diffusion through the semi-permeable membrane Spectra/Por® (Spectrum Laboratory, Gardena, CA, USA) and porcine ear skin. Moreover, a residual amount of drug in the skin after ex vivo diffusion was evaluated. The reference MER, lecithin-containing MEL, and gelatin-containing MEG were characterized in terms of their size, polydispersity index, density, viscosity, electrical conductivity and surface tension. Based on the in vitro diffusion, it can be argued that MEL slowed down the drug release, while MER and MEG have no significant effect compared to the sample, in which propylene glycol (PG) was used as a solubilizer. Determination of the residual drug amount in the skin after 6 h of the ex vivo permeation was demonstrated as the most valuable method to evaluate the effectiveness of the ME’s application. The results indicate that the most optimal MXD permeation enhancers in alginate gel were the natural surfactants containing MEs. MXD solubilization in MEG and MEL had caused more than 5% of the drug remaining in the skin, which is almost a 1.5-fold higher amount compared to the reference gel.

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Design and Development of Transdermal Patches of Antipsychotic Drug: In vitro and Ex vivo Characterization

International Journal of Applied Pharmaceutical Sciences and Research ◽

10.21477/ijapsr.5.3.2 ◽

2020 ◽

Vol 5 (03) ◽

pp. 45-53

Author(s):

Himabindu Peddapalli ◽

Anjaneyulu Rajagoni ◽

Preethi Pagilla ◽

Jerusha Perumala ◽

Shilpa Puppala ◽

...

Keyword(s):

Transient Stability ◽

Ex Vivo ◽

Hydroxypropyl Methylcellulose ◽

Research Work ◽

Content Uniformity ◽

Permeation Enhancers ◽

Drug Content ◽

Folding Endurance ◽

Eudragit Rl

The purpose of the present research work was to design, assess, and estimate the developed transdermal matrix-type formulation comprising levosulpiride hydrochloride with the objective of enhancing the bioavailability and compliance of the patient. Transdermal films of levosulpiride were developed using a solvent casting method by hydroxypropyl methylcellulose (HPMC) E 15, Eudragit RL 100, and Eudragit RS100. In current research work, propylene glycol and oleic acid was used as plasticizer and permeation enhancers in different fractions. Among the batches, drug content uniformity with all formulations was perceived between 91.6 to 98%. Folding endurance of patches was good and indicates satisfactory flexibility. Developed transdermal films had the necessary physicochemical properties, for example, uniformity of drug content, weight, thickness, folding endurance, and dampness content. Franz diffusion cell was used for in vitro diffusion studies utilizing dialysis membrane as a pervasion boundary. Formulation F5 (Eudragit RL 100-1%, HPMC E15-9%) was found to be best among all batches of its consistent release rate for 12 hours and the extent of drug release 97.76%. F5 was the most palatable formulation as it firmly meets the standards and continuously permeated drugs for 12 hours that can keep up desired therapeutic concentration in plasma. The patches were exposed to transient stability studies and were observed to be constant and stable.

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Effects of the Tibetan herbal preparation PADMA 28 on blood lipids and lipid oxidisability in subjects with mild hypercholesterolaemia

VASA ◽

10.1024/0301-1526.34.1.11 ◽

2005 ◽

Vol 34 (1) ◽

pp. 11-17 ◽

Cited By ~ 12

Author(s):

Brunner-La Rocca ◽

Schindler ◽

Schlumpf ◽

Saller ◽

Suter

Keyword(s):

Endothelial Dysfunction ◽

Blood Lipids ◽

Ex Vivo ◽

Hdl Cholesterol ◽

Blood Lipid ◽

Tibetan Medicine ◽

Double Blind ◽

Intraarterial Infusion ◽

Padma 28

Background: Previous studies showed an anti-atherosclerotic effect of PADMA 28, an herbal formula based on Tibetan medicine. As the mechanisms of action are not fully understood, we investigated whether PADMA 28 may lower blood lipids and lipid oxidisability, and affect early endothelial dysfunction. Patients and methods: Sixty otherwise healthy subjects with total cholesterol ≥5.2 mmol/l and < 8.0 mmol/l were randomly assigned to placebo or PADMA 28, 3 x 2 capsules daily, for 4 weeks (double-blind). Blood lipids (total, LDL-, and HDL-cholesterol, triglycerides, Apo-lipoprotein A1 and B) and ex vivo lipid oxidisability were measured before and after treatment. In a subset of 24 subjects, endothelial function was assessed using venous occlusion plethysmography with intraarterial infusion of acetylcholine. Isolated LDL and plasma both untreated and pre-treated with PADMA 28 extract were oxidised by the radical generator AAPH. Conjugated diene formation was measured at 245 nm. Results: Blood lipids did not change during the study in both groups. In contrast to previous reports in mild hypercholesterolaemia, no endothelial dysfunction was seen and, consequently, was not influenced by therapy. Ex vivo blood lipid oxidisability was significantly reduced with PADMA 28 (area under curve: 5.29 ± 1.62 to 4.99 ± 1.46, p = 0.01), and remained unchanged in the placebo group (5.33 ± 1.88 to 5.18 ± 1.78, p > 0.1). This effect persisted one week after cessation of medication. In vitro experiments confirmed the prevention of lipid peroxidation in the presence of PADMA 28 extracts. Persistent protection was also seen for LDL isolated from PADMA 28-pretreated blood after being subjected to rigorous purification. Conclusions: This study suggests that the inhibition of blood lipid oxidisability by PADMA 28 may play a role in its anti-atherosclerotic effect.

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The Role of Polyphenols in the Modulation of Plasma Non-Enzymatic Antioxidant Capacity (NEAC)

International Journal for Vitamin and Nutrition Research ◽

10.1024/0300-9831/a000116 ◽

2012 ◽

Vol 82 (3) ◽

pp. 228-232 ◽

Cited By ~ 7

Author(s):

Mauro Serafini ◽

Giuseppa Morabito

Keyword(s):

Antioxidant Capacity ◽

Dietary Intervention ◽

Ex Vivo ◽

The Body ◽

Dietary Polyphenols ◽

Enzymatic Antioxidant ◽

Endogenous Antioxidant

Dietary polyphenols have been shown to scavenge free radicals, modulating cellular redox transcription factors in different in vitro and ex vivo models. Dietary intervention studies have shown that consumption of plant foods modulates plasma Non-Enzymatic Antioxidant Capacity (NEAC), a biomarker of the endogenous antioxidant network, in human subjects. However, the identification of the molecules responsible for this effect are yet to be obtained and evidences of an antioxidant in vivo action of polyphenols are conflicting. There is a clear discrepancy between polyphenols (PP) concentration in body fluids and the extent of increase of plasma NEAC. The low degree of absorption and the extensive metabolism of PP within the body have raised questions about their contribution to the endogenous antioxidant network. This work will discuss the role of polyphenols from galenic preparation, food extracts, and selected dietary sources as modulators of plasma NEAC in humans.

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