Delivery of ethinylestradiol from film forming polymeric solutions across human epidermis in vitro and in vivo in pigs

2007 ◽  
Vol 118 (2) ◽  
pp. 196-203 ◽  
Author(s):  
Ines Zurdo Schroeder ◽  
Patrick Franke ◽  
Ulrich F. Schaefer ◽  
Claus-Michael Lehr
Pharmaceutics ◽  
2019 ◽  
Vol 11 (7) ◽  
pp. 310 ◽  
Author(s):  
Stella Zsikó ◽  
Kendra Cutcher ◽  
Anita Kovács ◽  
Mária Budai-Szűcs ◽  
Attila Gácsi ◽  
...  

The aim of this research was to investigate the stability of a lidocaine-loaded nanostructured lipid carrier dispersion at different temperatures, formulate a nanostructured lipid carrier gel, and test the penetration profile of lidocaine from the nanostructured lipid carrier gel using different skin penetration modeling methods. The formulations were characterized by laser diffraction, rheological measurements and microscopic examinations. Various in vitro methods were used to study drug release, diffusion and penetration. Two types of vertical Franz diffusion cells with three different membranes, including cellulose, Strat-M®, and heat separated human epidermis were used and compared to the Skin-parallel artificial membrane permeability assay (PAMPA) method. Results indicated that the nanostructured lipid carrier dispersion had to be gelified as soon as possible for proper stability. Both the Skin-PAMPA model and Strat-M® membranes correlated favorably with heat separated human epidermis in this research, with the Strat-M® membranes sharing the most similar drug permeability profile to an ex vivo human skin model. Our experimental findings suggest that even when the best available in vitro experiment is selected for modeling human skin penetration to study nanostructured lipid carrier gel systems, relevant in vitro/in vivo correlation should be made to calculate the drug release/permeation in vivo. Future investigations in this field are still needed to demonstrate the influence of membranes and equipment from other classes on other drug candidates.


Pharmaceutics ◽  
2019 ◽  
Vol 11 (8) ◽  
pp. 409 ◽  
Author(s):  
Yujin Kim ◽  
Moritz Beck-Broichsitter ◽  
Ajay Banga

Trolamine salicylate (TS) is a topical anti-inflammatory analgesic used to treat small joint pain. The topical route is preferred over the oral one owing to gastrointestinal side effects. In this study, a poly(lactide-co-glycolide) (PLGA)-based in situ bio-adhesive film-forming system for the transdermal delivery of TS was designed and evaluated. Therefore, varying amounts (0%, 5%, 10%, 20%, and 25% (w/w)) of PLGA (EXPANSORB® DLG 50-2A, 50-5A, 50-8A, and 75-5A), ethyl 2-cyanoacrylate, poly (ethylene glycol) 400, and 1% of TS were dissolved together in acetone to form the bio-adhesive polymeric solution. In vitro drug permeation studies were performed on a vertical Franz diffusion cell and dermatomed porcine ear skin to evaluate the distinct formulations. The bio-adhesive polymeric solutions were prepared successfully and formed a thin film upon application in situ. A significantly higher amount of TS was delivered from a formulation containing 20% PLGA (45 ± 4 µg/cm2) and compared to PLGA-free counterpart (0.6 ± 0.2 µg/cm2). Furthermore, the addition of PLGA to the polymer film facilitated an early onset of TS delivery across dermatomed porcine skin. The optimized formulation also enhanced the delivery of TS into and across the skin.


2017 ◽  
Vol 5 (9) ◽  
pp. 1868-1883 ◽  
Author(s):  
Sivalingam Udhayakumar ◽  
Krishnakumar Gopal Shankar ◽  
Sampath Sowndarya ◽  
Chellan Rose

The present study reports the development of a novel film-forming bovine collagenous cream (BCC) based on bovine collagen (BC).


1988 ◽  
Vol 107 (2) ◽  
pp. 427-446 ◽  
Author(s):  
A Stoler ◽  
R Kopan ◽  
M Duvic ◽  
E Fuchs

We report here the isolation and characterization of three antisera, each of which is specific for a single keratin from one of the three different pairs (K1/K10, K14/K5, K16/K6) that are differentially expressed in normal human epidermis and in epidermal diseases of hyperproliferation. We have used these antisera in conjunction with monospecific cRNA probes for epidermal keratin mRNAs to investigate pathways of differentiation in human epidermis and epidermal diseases in vivo and in epidermal cells cultured from normal skin and from squamous cell carcinomas in vitro. Specifically, our results suggest that: (a) the basal-specific keratin mRNAs are down-regulated upon commitment to terminal differentiation, but their encoded proteins are stable, and can be detected throughout the spinous layers; (b) the hyperproliferation-associated keratin mRNAs are expressed at a low level throughout normal epidermis when their encoded proteins are not expressed, but are synthesized at high levels in the suprabasal layers of hyperproliferating epidermis, coincident with the induced expression of the hyperproliferation-associated keratins in these cells; and (c) concomitantly with the induction of the hyperproliferation-associated keratins in the suprabasal layers of the epidermis is the down-regulation of the expression of the terminal differentiation-specific keratins. These data have important implications for our understanding of normal epidermal differentiation and the deviations from this process in the course of epidermal diseases of hyperproliferation.


2019 ◽  
Vol 9 (1) ◽  
Author(s):  
Samaneh Moghadasi Boroujeni ◽  
Alison Koontz ◽  
Georgios Tseropoulos ◽  
Laura Kerosuo ◽  
Pihu Mehrotra ◽  
...  

Author(s):  
NABIL ABDULLAH ◽  
AMIT B. PATIL

Objective: Voriconazole (VCZ) is a broad-spectrum antifungal medication that works by inhibiting fungal Cytochrome P450, preventing fungi growth. The current study aims at developing and characterizing an antifungal in situ film-forming polymeric solution spray containing VCZ for use in topical drug delivery systems. Methods: Optimized VCZ in situ polymeric film formulation was evaluated for Fourier transform infrared spectroscopy (FTIR), differential scanning calorimeter (DSC), X-ray diffractometry (XRD), Scanning electron microscope (SEM), in vitro and in vivo, ex-vivo investigation using abdominal rat skin and stability studies. The in vivo antifungal activity of the advanced in situ film was examined in albino Wistar rats. Results: The optimized batch contained 22% Eudragit RS 100 (ERS) and 4% Sorbitol. Based on FTIR, XRD, SEM, and rheological studies. Formulation ingredients of VCZ loaded topical in situ polymeric film spray were observed to be compatible and showed no evidence of precipitation, deformation, or discoloration. Diffusion test (in vitro %), and ex-vivo drug diffusion % obtained 99.22%, and 97.45% respectively. The maximum inhibition zone was measured at 13±0.07 mm. The Wistar rat was employed as an animal model for skin irritation and antifungal studies. A study of short-term stability observed no significant modifications in the physical properties. Conclusion: The findings of the optimized VCZ topical in situ polymeric film spray formulation were satisfactory, demonstrating comparable improvement in superficial antifungal treatment.


Author(s):  
Narayan Sahoo ◽  
Bhabani Satapathy ◽  
Subrata Mallick

The objective of the present work was to investigate the effect of various hydrophilic polymers like hydroxypropylmethyl cellulose, methyl cellulose, carboxymethyl cellulose and poly vinyl alcohol on the in vitro dissolution property of ibuprofen (IBU) crystallized from aqueous polymeric solutions. By using solvent-change technique, IBU crystal products were produced in presence of the selected polymers. Results showed that in presence of polymers; crystallization yield of IBU was higher than that of pure drug crystal (absence of polymer). SEM photographs revealed visible changes in the crystal morphology in the presence of polymers. The FTIR spectra of the crystallized IBU (polymer-treated) showed a shifting of the acid-dimer peak from 1718 cm-1 to 1721 cm-1 but absence of specific peaks for polymers. XRD study further confirmed absence of polymers in the crystallized IBU as no specific peaks were observed for the polymers. A higher percentage of cumulative drug release was reported for the polymeric-treated IBU crystals than that of plain IBU. Further in vivo studies are warranted to establish the in vitro-in vivo correlation for the future technology transfer of the formulation.


Drug Delivery ◽  
2017 ◽  
Vol 24 (1) ◽  
pp. 1056-1066 ◽  
Author(s):  
Dong-Won Oh ◽  
Ji-Hyun Kang ◽  
Hyo-Jung Lee ◽  
Sang-Duk Han ◽  
Min-Hyung Kang ◽  
...  

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