Evaluation of in vitro/in vivo correlations for three fentanyl transdermal delivery systems using in vitro skin permeation testing and human pharmacokinetic studies under the influence of transient heat application

2021 ◽  
Author(s):  
Soo Hyeon Shin ◽  
Mingming Yu ◽  
Dana C. Hammell ◽  
Priyanka Ghosh ◽  
Sam G. Raney ◽  
...  
Keyword(s):  
Transdermal Delivery ◽  
Skin Permeation ◽  
Delivery Systems ◽  
Pharmacokinetic Studies ◽  
Human Pharmacokinetic ◽  
In Vitro Skin Permeation ◽  
Heat Application

Transdermal Delivery of Metoprolol II: In-Vitro Skin Permeation and Bioavailability in Hairless Rats

1995 ◽  
Vol 84 (2) ◽  
pp. 158-160 ◽  
Author(s):  
Tapash K. Ghosh ◽  
Joseph Adir ◽  
Si‐Ling Xiang ◽  
Samuel Onyilofur
Keyword(s):  
Transdermal Delivery ◽  
Skin Permeation ◽  
In Vitro Skin Permeation

scholarly journals Antimicrobial Activity of Non-steroidal Anti-inflammatory Drugs on Biofilm: Current Evidence and Potential for Drug Repurposing

2021 ◽  
Vol 12 ◽  
Author(s):  
Rodrigo Cuiabano Paes Leme ◽  
Raquel Bandeira da Silva
Keyword(s):  
Bacterial Species ◽  
Drug Repurposing ◽  
Current Evidence ◽  
Pharmacokinetic Studies ◽  
Bacterial Populations ◽  
Human Pharmacokinetic ◽  
Inflammatory Drugs ◽  
Anti Inflammatory

It has been demonstrated that some non-steroidal anti-inflammatory drugs (NSAIDs), like acetylsalicylic acid, diclofenac, and ibuprofen, have anti-biofilm activity in concentrations found in human pharmacokinetic studies, which could fuel an interest in repurposing these well tolerated drugs as adjunctive therapies for biofilm-related infections. Here we sought to review the currently available data on the anti-biofilm activity of NSAIDs and its relevance in a clinical context. We performed a systematic literature review to identify the most commonly tested NSAIDs drugs in the last 5 years, the bacterial species that have demonstrated to be responsive to their actions, and the emergence of resistance to these molecules. We found that most studies investigating NSAIDs’ activity against biofilms were in vitro, and frequently tested non-clinical bacterial isolates, which may not adequately represent the bacterial populations that cause clinically-relevant biofilm-related infections. Furthermore, studies concerning NSAIDs and antibiotic resistance are scarce, with divergent outcomes. Although the potential to use NSAIDs to control biofilm-related infections seems to be an exciting avenue, there is a paucity of studies that tested these drugs using appropriate in vivo models of biofilm infections or in controlled human clinical trials to support their repurposing as anti-biofilm agents.

Formulation and Characterization of Transethosomes for Enhanced Transdermal Delivery of Propranolol Hydrochloride

2020 ◽  
Vol 12 (1) ◽  
pp. 38-47 ◽  
Author(s):  
Lalit Kumar ◽  
Puneet Utreja
Keyword(s):  
Plasma Concentration ◽  
Skin Permeation ◽  
Laser Scanning Microscopy ◽  
Prolonged Release ◽  
Propranolol Hydrochloride ◽  
Oral Tablet ◽  
In Vitro Skin Permeation ◽  
Oral Propranolol

Objective: The objective of the present work was to develop transethosomes loaded with propranolol hydrochloride using Lipoid S100 as phospholipid, and oleic acid as permeation enhancer and evaluate them for prolonged release effect, in-vitro skin permeation, and in-vivo plasma concentration. Methods: Transethosomes loaded with propranolol hydrochloride were prepared by homogenization method. Furthermore, they were characterized by using Transmission Electron Microscopy (TEM), zeta sizer, Differential Scanning Calorimetry (DSC), and Confocal Laser Scanning Microscopy (CLSM) for in-vitro skin permeation. Plasma concentration profile of transethosomal gel was determined using Sprague Dawley rats and compared with a marketed oral tablet of propranolol hydrochloride. Results: Developed transethosomes loaded with propranolol hydrochloride showed acceptable size (182.7 ± 5.4 nm), high drug entrapment (81.98 ± 2.9%) and good colloidal characteristics [polydispersity index (PDI) = 0.234 ± 0.039, zeta potential = -21.91 ± 0.65 mV]. Transethosomes showed prolonged in-vitro release of propranolol hydrochloride for 24 h. Results of in-vitro skin permeation studies of transethosomal gel showed 74.34 ± 2.33% permeation of propranolol hydrochloride after 24 h and confocal microscopy revealed accumulation of transethosomes in the stratum basale layer of the skin. Transethosomal gel was capable to prolong the in-vivo release of propranolol hydrochloride upto 24 h. The value of peak plasma concentration (Cmax) of propranolol hydrochloride was found to be 93.8 ± 3.6 ng/mL which was very high compared to the marketed oral tablet of propranolol hydrochloride (45.6 ± 3.1 ng/mL). Conclusion: The results suggested that transethosomal gel of propranolol hydrochloride could be a better alternative to oral propranolol hydrochloride as it can avoid various disadvantages of oral propranolol hydrochloride like high dosing frequency, first pass effect, and organ toxicity.

scholarly journals Ondansetron HCl Microemulsions for Transdermal Delivery: Formulation and In Vitro Skin Permeation

2012 ◽  
Vol 2012 ◽  
pp. 1-6 ◽  
Author(s):  
Jadupati Malakar ◽  
Amit Kumar Nayak ◽  
Aalok Basu
Keyword(s):  
Transdermal Delivery ◽  
Isopropyl Alcohol ◽  
Skin Permeation ◽  
Tween 80 ◽  
Oral Route ◽  
Isopropyl Myristate ◽  
Surfactant Phase ◽  
In Vitro Skin Permeation ◽  
Pass Metabolism

Ondansetron HCl delivery through oral route suffers due to its low bioavailability due to first-pass metabolism. Therefore, the microemulsion-based transdermal delivery may be a better substitute for it. The pseudoternary phase diagrams were constructed to determine compositions of microemulsions, and ondansetron HCl microemulsions for transdermal delivery were developed using isopropyl myristate or oleic acid as the oil phase, Tween 80 as the surfactant, and isopropyl alcohol as the cosurfactant evaluated for in vitro skin permeation through excised porcine skin. The in vitro skin permeation from these formulated microemulsions was sustained over 24 hours. The microemulsion F-8 (contained 10% of isopropyl myristate as oil phase, 8% of aqueous phase, and 82% of surfactant phase containing Tween 80 and isopropyl alcohol, 3 : 1) showed the highest permeation flux of 0.284±0.003 μg/cm2/hour. All these microemulsions followed the Korsmeyer-Peppas model (R2=0.971  to  0.998) with non-Fickian, “anomalous” mechanism over a period of 24 hours.

scholarly journals Okra-Thioglycolic Acid Conjugate—Synthesis, Characterization, and Evaluation as a Mucoadhesive Polymer

Processes ◽  
2020 ◽  
Vol 8 (3) ◽  
pp. 316 ◽  
Author(s):  
N. Raghavendra Naveen ◽  
Chakka Gopinath ◽  
Mallesh Kurakula
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Delivery Systems ◽  
Pharmacokinetic Studies ◽  
Natural Polymers ◽  
Covalent Bonds ◽  
Prolonged Contact ◽  
Thiol Functionalization

The success of mucoadhesive drug delivery systems relies on the type of polymer used, which becomes adhesive naturally upon hydration. Intended polymers should be able to maintain prolonged contact with biological membranes, and to protect or cater the drug to a prolonged period. Most of the hydro polymers form weak non-covalent bonds, that hinder localization of dosage forms at specific sites resulting in therapeutic inefficiency. This can be overcome by the thiol functionalization of natural polymers. In the present study, natural okra gum (OG) was extracted, followed by thiolation (TOG) and evaluated for mucoadhesion property and its role in enhancing the efficacy of repaglinide as a model drug (short-acting Type II antidiabetic drug). The thiol functionalization of OG (TOG) was confirmed by a Fourier-transform infrared spectroscopy (FTIR) study that showed a polyhedral to a spherical shape that had a rougher surface. Differential scanning calorimetry (DSC) and X-Ray Diffraction (XRD) studies of TOG indicated a decline in endothermic transition temperature and high crystallinity, respectively, in comparison to OG. CSFR (Crushing Strength: Friability Ratio), weight and thickness variations of repaglinidetablets formulated using TOG were >80% and <2.5% respectively. The highest swelling index (107.89 ± 1.99%) and strong mucoadhesion due to high disulfide bonds were observed for repaglinide TOG tablets in comparison to RG OG tablets. In-vitro release studies indicated a controlled drug release from thiolated formulations proportional to the concentration of thiomers that have a good correlation with in-vivo studies. Pharmacokinetic studies indicated higher AUC (area under the curve), longer t1/2 with thiomers. and Level A IVIV (in vitro in vivo) correlation was established from the bioavailability and dissolution data. Consequently, all the obtained results suggest that thiomers based formulations can be promising drug delivery systems, even in targeting onerous mucosal surfaces like nasal, ocular or vaginal.

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