In vitro – in vivo correlations for nicotine transdermal delivery systems evaluated by both in vitro skin permeation (IVPT) and in vivo serum pharmacokinetics under the influence of transient heat application

2018 ◽  
Vol 270 ◽  
pp. 76-88 ◽  
Author(s):  
Soo Hyeon Shin ◽  
Sherin Thomas ◽  
Sam G. Raney ◽  
Priyanka Ghosh ◽  
Dana C. Hammell ◽  
...  
1995 ◽  
Vol 84 (2) ◽  
pp. 158-160 ◽  
Author(s):  
Tapash K. Ghosh ◽  
Joseph Adir ◽  
Si‐Ling Xiang ◽  
Samuel Onyilofur

2020 ◽  
Vol 12 (1) ◽  
pp. 38-47 ◽  
Author(s):  
Lalit Kumar ◽  
Puneet Utreja

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.


2012 ◽  
Vol 2012 ◽  
pp. 1-6 ◽  
Author(s):  
Jadupati Malakar ◽  
Amit Kumar Nayak ◽  
Aalok Basu

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.


1998 ◽  
Vol 175 (1) ◽  
pp. 85-94 ◽  
Author(s):  
Antonella Saija ◽  
Antonio Tomaino ◽  
Domenico Trombetta ◽  
Marcella Giacchi ◽  
Anna De Pasquale ◽  
...  

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