Formulation and Ex-vivo Evaluation of Transdermal Patches of Glipizide using the Penetration Enhancer Buchanania- Lanzan (Spreng) Seed Oil

2015 ◽  
Vol 8 (1) ◽  
pp. 2768-2774
Author(s):  
Sudarshan Singh ◽  
Sunil B Bothara ◽  
D. Roshan Patel ◽  
Mahobia K Naveen
Keyword(s):  
Essential Oils ◽  
Seed Oil ◽  
Ex Vivo ◽  
Drug Loading ◽  
Penetration Enhancers ◽  
Permeation Enhancement ◽  
Dsc Studies ◽  
Transdermal Patches ◽  
Effective Stability

The aim of the present work was to evaluate the permeation enhancement properties of Buchanania lanzan spreng seed oil. Ethyl cellulose transdermal patches of Glipizide using some essential oils as penetration enhancers were developed. Effect of drug loading and penetration enhancers on the in vitro permeation of drug through rat skin was investigated. Incorporation of essential oils enhanced the moisture content, moisture uptake capacity and permeation of Glipizide across skin barriers. Among the penetration enhancers used, Buchanania lanzan spreng seed oil found to be most effective. Stability as well FTIR and DSC studies did not show any Interaction/degradation of the drug. It was concluded that stable and effective Glipizide transdermal patches can be prepared using essential oils as penetration enhancers. Further it was also concludes that the seed oil can be used in permeation enhancement of various types of tropical preparation.  

scholarly journals Polishing the Therapy of Onychomycosis Induced by Candida spp.: Amphotericin B–Loaded Nail Lacquer

Pharmaceutics ◽  
2021 ◽  
Vol 13 (6) ◽  
pp. 784
Author(s):  
Aleph M. S. Souza ◽  
Renato C. A. Ribeiro ◽  
Gleyse K. L. O. Pinheiro ◽  
Francisco I. Pinheiro ◽  
Wógenes N. Oliveira ◽  
...  
Keyword(s):  
Amphotericin B ◽  
Ex Vivo ◽  
Drug Loading ◽  
Drug Bioavailability ◽  
Candida Spp ◽  
Drying Time ◽  
Analytical Method Validation ◽  
Nail Lacquer ◽  
In Vitro Adhesion

Onychomycosis induced by Candida spp. has several limitations regarding its treatment. Nail lacquers display the potential to overcome these drawbacks by providing therapeutic compliance and increasing local drug bioavailability. Thus, this work aimed to produce a nail lacquer loaded with Amphotericin B (AmB) and evaluate its performance. The AmB-loaded nail lacquer was produced and preliminarily characterized. An AmB quantification method was developed. Stability, drug release, permeability and anti-Candida activity assays were conducted. The analytical method validation met the acceptance criteria. The drug loading efficiency was 100% (0.02 mg/g of total product), whereas the AmB stability was limited to ≅ 7 days (≅ 90% remaining). The nail lacquer displayed a drying time of 187 s, non-volatile content of around 20%w/w, water-resistance of approximately 2%w/w of weight loss and satisfactory in vitro adhesion. Moreover, the in vitro antifungal activity against different Candida spp. strains was confirmed. The AmB release and the ex vivo permeability studies revealed that AmB leaves the lacquer and permeates the nail matrix in 47.76 ± 0.07% over 24 h. In conclusion, AmB-loaded nail lacquer shows itself as a promising extemporaneous dosage form with remarkable anti-Candida activity related to onychomycosis.

scholarly journals Preparation and Evaluation of Matrix Type Transdermal Patches of Domperidone Maleate: in vitro and ex vivo Characterization

2017 ◽  
Vol 51 (4) ◽  
pp. 517-524
Author(s):  
Suddala Shirisha ◽  
Gomathi Joshi ◽  
Sunit Kumar Sahoo ◽  
Yamsani Madhusudan Rao
Keyword(s):  
Ex Vivo ◽  
Matrix Type ◽  
Transdermal Patches ◽  
Preparation And Evaluation

scholarly journals Bioassay-guided optimization of lipid-based erythromycin microparticles

2020 ◽  
Vol 19 (7) ◽  
pp. 1351-1358
Author(s):  
Ifeanyi T. Nzekwe ◽  
Anselm C. Okere ◽  
Ifeanyi E. Okoye ◽  
Kokonne E. Ekere ◽  
Adaobi A. Ezenwa ◽  
...  
Keyword(s):  
Ex Vivo ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Antimicrobial Activities ◽  
Hydrodynamic Size ◽  
Chemical Assay ◽  
Acid Ratio ◽  
Drug Entrapment Efficiency ◽  
Lower Variation

Purpose: To optimize erythromycin microparticles by in vitro bioassay methods based on its antibacterial activity. Methods: The microparticles were produced by high shear homogenization. The effects of different lipid-to-surfactant ratios were studied. The hydrodynamic size of the different batches was evaluated using dynamic light scattering while bioactive drug load per batch was assessed in agar using bioassay methods. The antimicrobial activities of selected batches were tested ex vivo by determination of reduction in bacteraemia following administration of the microparticles to infected animals. Results: All batches had particles with hydrodynamic sizes < 8.5 microns. Batch 7 with a 2: 5: 2.5 (drug: surfactant: stearic acid) ratio, represents the optimized batch with a hydrodynamic size of 2281 nm, a bioactive drug loading capacity (BLC) of 4.67 ± 0.70 % and bioactive drug entrapment  efficiency (BEE) of 10.51 %. The “microparticle MIC” against Staphylococcus aureus was 1.74 x 10-3 μg/ml. Despite containing lower amounts of erythromycin than the pure sample, the microparticles achieved comparable reduction in bacteraemia, with the optimized batch exhibiting lower variation in bacteraemia than the pure drug. Conclusion: Erythromycin microparticles have been successfully optimized with the aid of bioassay methods which has the advantage that only the bioactive drug concentration is factored in. This method eliminates problems posed by inadequate or non-discriminating chemical assay methods. Keywords: Microparticles, Erythromycin, Gastrointestinal, Bioavailability Antimicrobial, Bioactivity, Encapsulation

Safety and efficacy of combined essential oils for the skin barrier properties: in vitro , ex vivo and clinical studies

2022 ◽  
Author(s):  
VHP Infante ◽  
PMBG Maia Campos ◽  
LR Gaspar¹ ◽  
ME Darvin ◽  
J Schleusener ◽  
...  
Keyword(s):  
Essential Oils ◽  
Clinical Studies ◽  
Ex Vivo ◽  
Skin Barrier ◽  
Barrier Properties ◽  
Safety And Efficacy

Antimicrobial potential of irrigants based on essential oils of Cymbopogon martinii and Thymus zygis towards in vitro multispecies biofilm cultured in ex vivo root canals

2020 ◽  
Vol 117 ◽  
pp. 104842
Author(s):  
Jelena Marinković ◽  
Dragana Mitić Ćulafić ◽  
Biljana Nikolić ◽  
Stefana Đukanović ◽  
Tatjana Marković ◽  
...  
Keyword(s):  
Essential Oils ◽  
Ex Vivo ◽  
Root Canals ◽  
Antimicrobial Potential ◽  
Multispecies Biofilm ◽  
Thymus Zygis ◽  
Cymbopogon Martinii

scholarly journals Essential Oils as Components of a Diet-Based Approach to Management of Helicobacter Infection

2003 ◽  
Vol 47 (10) ◽  
pp. 3240-3246 ◽  
Author(s):  
G. E. Bergonzelli ◽  
D. Donnicola ◽  
N. Porta ◽  
I. E. Corthésy-Theulaz
Keyword(s):  
Essential Oils ◽  
Seed Oil ◽  
Oral Treatment ◽  
Food Additives ◽  
Peptic Ulcers ◽  
Carrot Seed ◽  
Bactericidal Activities ◽  
H Pylori

ABSTRACT An increased density of Helicobacter pylori in the gastric mucosa can be associated with more severe gastritis and an increased incidence of peptic ulcers. Therefore, people with asymptomatic gastritis would certainly benefit from a nutritional approach to help them manage the infection and therefore decrease the risk of development of associated pathologies. We analyzed the activities of 60 essential oils against H. pylori P1 and identified 30 oils that affected growth, with in vitro inhibition zones ranging between 0.7 and 6.3 cm in diameter. We further analyzed the effects of 16 oils with different activities on H. pylori P1 viability. Fifteen showed strong bactericidal activities, with minimal bactericidal concentrations after 24 h ranging from 0.02 to 0.1 g/liter at pH 7.4. Even though slight variations in activities were observed, the essential oils that displayed the strongest bactericidal potentials against H. pylori P1 were also active against other Helicobacter strains tested. Among the pure constituents of different essential oils tested, carvacrol, isoeugenol, nerol, citral, and sabinene exhibited the strongest anti-H. pylori activities. Although oral treatment of H. pylori SS1-infected mice with carrot seed oil did not result in significant decreases in the bacterial loads in the treated animals compared to those in the control animals, in all experiments performed, the infection was cleared in 20 to 30% of carrot seed oil-treated animals. Our results indicate that essential oils are unlikely to be efficient anti-Helicobacter agents in vivo. However, their effects may not be irrelevant if one plans to use them as food additives to complement present therapies.

scholarly journals Transdermal Delivery of Telmisartan: Formulation, in vitro, ex vivo, Iontophoretic Permeation Enhancement and Comparative Pharmacokinetic Study in Rats

2021 ◽  
Vol Volume 15 ◽  
pp. 4603-4614
Author(s):  
Mahmoud Teaima ◽  
Rehab Abdelmonem ◽  
Yomna A Adel ◽  
Mohamed A El-Nabarawi ◽  
Tayseer M El-Nawawy
Keyword(s):  
Pharmacokinetic Study ◽  
Transdermal Delivery ◽  
Ex Vivo ◽  
Comparative Pharmacokinetic ◽  
Permeation Enhancement

scholarly journals FORMULATION AND EVALUATION OF TRANSDERMAL PATCHES OF METOPROLOL TARTRATE USING PERMEATION ENHANCERS OF NATURAL AND SYNTHETIC ORIGIN

2019 ◽  
pp. 317-323
Author(s):  
SHIKHA BAGHEL CHAUHAN ◽  
SUSHILA SAINI
Keyword(s):  
Moisture Absorption ◽  
Skin Permeation ◽  
Penetration Enhancers ◽  
Moisture Loss ◽  
Metoprolol Tartrate ◽  
Peg 400 ◽  
Transdermal Patches ◽  
Weight Variation ◽  
Basil Oil

Objective: Oral metoprolol tartrate has a short elimination half-life (2-3h) and low bioavailability undergoes extensive first-pass metabolism and frequent dosing. The aim of the present investigation was to formulate, develop and evaluate metoprolol tartrate transdermal patches using various synthetic and natural penetration enhancers. Methods: Enhancers used were eugenol, limonene, basil oil, urea and SLS (sodium lauryl sulphate). Polymer used was chitosan and PEG 400 used as a plasticizer. Transdermal Films were prepared by using solvent casting method. FTIR and DSC were studied to assess any interaction between the drug and polymers. Films were evaluated for Physico-chemical Characteristics like thickness, weight variation, folding endurance, moisture loss, moisture absorption and drug content. In vitro skin permeation studies were performed using Keshary chien cell For 24 h across rat skin. Results: Chitosan was found to be a suitable polymer for matrix formation. 3.5% w/w was used to optimize to formulate transdermal patches. 1.5% of total solution v/v lactic acid was used for dissolution of chitosan. 2.5%v/v of total solution PEG 400 was used to provide plasticity and smoothness to the patches. From the evaluation of patches formulation, F10 containing Basil oil as penetration enhancer in the concentration of 1.5% v/v was found to be best among all batches because of its consistent release rate For 24 h and extent of drug release was 85.20%. It can be concluded that naturally occurring volatile oils i.e., terpenes appear acceptable permeation enhancer and shows the best permeation across skin as indicated by high percutaneous enhancement ability. Conclusion: The developed transdermal patches are stable, non-irritating, and had increased efficacy of metoprolol and therefore had a good potential for hypertension treatment.

DESIGN AND IN VITRO EVALUATION OF MUCOADHESIVE BUCCAL FILMS OF LERCANIDIPINE HCL

INDIAN DRUGS ◽  
2013 ◽  
Vol 50 (07) ◽  
pp. 31-40
Author(s):  
H. Doddayya ◽  
◽  
S.S Patil ◽  
M Suman ◽  
P Kumar ◽  
...  
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Release Mechanism ◽  
In Vitro Drug Release ◽  
Dsc Studies ◽  
Zero Order Kinetics ◽  
Accelerated Stability ◽  
Buccal Films ◽  
Lercanidipine Hydrochloride

Lercanidipine hydrochloride, an anti hypertension drug, undergoes extensive first pass metabolism to inactive metabolites leading to very poor oral bioavailability. To overcome this problem, buccal films of Lercanidipine hydrochloride were prepared by solvent casting method, employing HPMC, HPC (alone and in combination with PVP) and PVP K30. The film thickness, weight, folding endurance, mucoadhesive strength and time were dependent on the nature and concentration of polymers used. The optimized film (F12, HPMC 3% and PVP 1.5%) showed: Swelling index (51.26 ± 1.90 %), ex vivo mucoadhesive strength (12.64 ± 0.83 grams) and time (3.6 ± 0.5hrs). In vitro drug release was inversely proportional to the polymeric concentration. Ex- vivo drug release studies carried out using goat buccal membrane was slower (42.90%, 6 hrs) compared to in vitro drug release (74.2%, 8hrs) for the same formulation (F12). The drug release mechanism for the optimized formulation followed zero order kinetics. FT-IR and DSC studies revealed the absence of any interaction between the formulation ingredients. The films remained stable during the accelerated stability conditions.

Mucoadhesive PEGylated inulin-based self-assembling nanoparticles: In vitro and ex vivo transcorneal permeation enhancement of corticosteroids

2019 ◽  
Vol 49 ◽  
pp. 195-208 ◽  
Author(s):  
Giulia Di Prima ◽  
Flavia Bongiovì ◽  
Fabio Salvatore Palumbo ◽  
Giovanna Pitarresi ◽  
Mariano Licciardi ◽  
...  
Keyword(s):  
Ex Vivo ◽  
Permeation Enhancement ◽  
Self Assembling
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