In vivo and in vitro Skin Permeation of Butyl Methoxydibenzoylmethane from Lipospheres

2008 ◽  
Vol 21 (1) ◽  
pp. 30-38 ◽  
Author(s):  
V. Iannuccelli ◽  
G. Coppi ◽  
S. Sergi ◽  
M. Mezzena ◽  
S. Scalia
Keyword(s):  
Skin Permeation ◽  
In Vitro Skin Permeation

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.

Preparation of osthole-loaded nano-vesicles for skin delivery: Characterization, in vitro skin permeation and preliminary in vivo pharmacokinetic studies

2016 ◽  
Vol 92 ◽  
pp. 49-54 ◽  
Author(s):  
Shu Meng ◽  
Chong Zhang ◽  
Wei Shi ◽  
Xiao‑Wei Zhang ◽  
Dan‑Hua Liu ◽  
...  
Keyword(s):  
Skin Permeation ◽  
Pharmacokinetic Studies ◽  
Skin Delivery ◽  
In Vitro Skin Permeation

Influence of different penetration enhancers on in vitro skin permeation and in vivo photoprotective effect of flavonoids

1998 ◽  
Vol 175 (1) ◽  
pp. 85-94 ◽  
Author(s):  
Antonella Saija ◽  
Antonio Tomaino ◽  
Domenico Trombetta ◽  
Marcella Giacchi ◽  
Anna De Pasquale ◽  
...  
Keyword(s):  
Skin Permeation ◽  
Penetration Enhancers ◽  
In Vitro Skin Permeation

scholarly journals Design and optimization of nano invasomal gel of Glibenclamide and Atenolol combination: in vitro and in vivo evaluation

2021 ◽  
Vol 7 (1) ◽  
Author(s):  
P. Anitha ◽  
S. V. Satyanarayana
Keyword(s):  
Disease Risk ◽  
Skin Permeation ◽  
Skin Irritation ◽  
Entrapment Efficiency ◽  
Noncommunicable Disease ◽  
In Vivo Evaluation ◽  
Design And Optimization ◽  
In Vitro Skin Permeation

Abstract Background There are many circumstances where chronic disease is associated with other disorders, especially in diseases such as diabetes with noncommunicable disease risk factors, such as hypertension. The current therapies for treating such chronic comorbid diseases are limited and challenging due to the difficulties in overcoming the side effects from complex therapeutic treatment regimen. The present study is aimed to develop and optimize the combinational nano invasomal gel of Glibenclamide (GLB) and Atenolol (ATN) as a novel combination therapy for comorbid treatment of diabetic hypertensive patients. The developed formulations were characterized for various parameters, including in-vitro skin permeation, skin irritation, in-vivo antidiabetic, and antihypertensive activities. Results OCNIG showed that the % entrapment efficiency of GLB is 96.67 ± 0.65% and % entrapment efficiency of ATN is 93.76 ± 0.89%, flux of GLB (240.43 ± 1.76 μg/cm2/h), and flux of ATN (475.2 ± 1.54 μg/cm2/h) which was found to conform to the expected value. The results indicated desired release and permeation profiles. Optimized formulation showed significant pharmacokinetic properties, which shows improvement in bioavailability by 134.30% and 180.32% respectively for two drugs, when compared to marketed oral preparation. Pharmacodynamic studies showed improved and prolonged management of diabetes and hypertension in Wistar rats, compared to oral and drug-loaded nano invasomes formulations. Conclusion Overall, the results showed that nano invasomal gel was found to be a useful and promising transdermal delivery system for the treatment of concurrent diseases.

Application of Box–Behnken design for preparation of glibenclamide loaded lipid based nanoparticles: Optimization, in vitro skin permeation, drug release and in vivo pharmacokinetic study

2016 ◽  
Vol 219 ◽  
pp. 897-908 ◽  
Author(s):  
Mohammed Aslam ◽  
Mohd. Aqil ◽  
Abdul Ahad ◽  
Abul Kalam Najmi ◽  
Yasmin Sultana ◽  
...  
Keyword(s):  
Drug Release ◽  
Pharmacokinetic Study ◽  
Skin Permeation ◽  
Box Behnken Design ◽  
In Vitro Skin Permeation

In Vitro Skin Permeation Methodology for Over-The-Counter Topical Dermatologic Products

2019 ◽  
pp. 216847901987533 ◽  
Author(s):  
Luke Oh ◽  
Sojeong Yi ◽  
Da Zhang ◽  
Soo Hyeon Shin ◽  
Edward Bashaw
Keyword(s):  
Product Life Cycle ◽  
Skin Permeation ◽  
Systemic Exposure ◽  
Skin Permeability ◽  
Over The Counter ◽  
In Vitro Permeation ◽  
In Vitro Skin Permeation ◽  
Study Sites

For topically applied over-the-counter (OTC) products, the association of unwanted systemic exposure and adverse events may be difficult to ascertain without a recognition or determination of in vivo absorption. Evaluation of skin permeability using a validated in vitro permeation methodology can provide important information for both initial formulation selection and reformulation during the product life cycle. Additionally, a comparison of permeation rates between formulations using a validated methodology could reduce the number of nonclinical studies needed as part of reformulation. However, many in vitro permeation tests (IVPTs) have produced results with high variability and low reproducibility between study sites. It is unclear if this is due to a lack of a standardized protocol, or lack of control of multiple key experimental factors including skin source, preparation, receptor fluid, and study design. This review presents the authors perspective on the potential regulatory utility of IVPT and proposes steps to improve the accuracy and reproducibility of IVPT. The focus of this review is on topical dermatologic drugs with an initial emphasis on the OTC marketplace where reformulations are more common.

Sign in / Sign up

Export Citation Format

Share Document