scholarly journals Viscosified Solid Lipidic Nanoparticles Based on Naringenin and Linolenic Acid for the Release of Cyclosporine A on the Skin

Molecules ◽  
2020 ◽  
Vol 25 (15) ◽  
pp. 3535
Author(s):  
Sonia Trombino ◽  
Camilla Servidio ◽  
Annarita Stella Laganà ◽  
Filomena Conforti ◽  
Mariangela Marrelli ◽  
...  
Keyword(s):  
Side Effects ◽  
Linolenic Acid ◽  
Skin Permeation ◽  
Systemic Absorption ◽  
Psoriasis Treatment ◽  
Potential Applications ◽  
In Vitro Skin Permeation ◽  
Systemic Side Effects ◽  
Lipophilicity Potential

Psoriasis is one of the most common human skin disorders. Although its pathogenesis is complex and not completely know, the hyperactivation of the immune system seem to have a key role. In this regard, among the most effective systemic therapeutics used in psoriasis, we find cyclosporine, an immunosuppressive medication. However, one of the major problems associated with the use of cyclosporine is the occurrence of systemic side effects such as nephrotoxicity, hypertension, etc. The present work fits in this context and its aim is the design of suitable platforms for cyclosporine topical release in psoriasis treatment. The main objective is to achieve local administration of cyclosporine in order to reduce its systemic absorption and, consequently, its side effects. In order to improve dermal penetration, solid lipid nanoparticles (SLNs) are used as carriers, due to their lipophilicity and occlusive properties, and naringenin and linolenic acid are chosen, due to their properties, as starting materials for SLNs design. In order to have dermatological formulations and further modulate drug release, SLNs are incorporated in several topical vehicles obtaining gels with different degree of lipophilicity. Potential applications for psoriasis treatment were evaluated by considering the encapsulation efficiency, release profiles, in vitro skin permeation, and anti-inflammatory effects.

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

In vitro skin permeation of buprenorphine transdermal patch

2020 ◽  
Vol 16 (6) ◽  
Author(s):  
C.-L. Liao ◽  
C.-C. Huang ◽  
C.-Y. Lee ◽  
T.-H. Chiu ◽  
S.-C. Kuo ◽  
...  
Keyword(s):  
Skin Permeation ◽  
Transdermal Patch ◽  
In Vitro Skin Permeation

scholarly journals FORMULATION AND DEVELOPMENT OF TRANSDERMAL DRUG DELIVERY SYSTEM OF ETHINYLESTRADIOL AND TESTOSTERONE: IN VITRO EVALUATION

2019 ◽  
Vol 11 (1) ◽  
pp. 55
Author(s):  
Shikha Baghel Chauhan ◽  
Tanveer Naved ◽  
Nayyar Parvez
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Transdermal Drug Delivery ◽  
Skin Permeation ◽  
Physical Parameters ◽  
Transdermal Patch ◽  
Transdermal Drug Delivery System ◽  
In Vitro Skin Permeation

Objective: The combination therapy of ethinylestradiol and testosterone in post-menopausal females has shown improved sexual response and libido. The present studies were designed to develop a suitable matrix-type transdermal drug delivery system (TDDS) of ethinylestradiol and testosterone using the polymer chitosan.Methods: Five formulations (ET1 to ET5) were developed by varying the concentration of polymer and keeping the drug load constant. Physical parameters and drug excipient interaction studies were evaluated in all the formulations. In vitro skin permeation profiles of ethinylestradiol and testosterone from various formulations were simultaneously characterized in a thermostatically controlled modified Franz Diffusion cell using HPLC. Based on the physical parameters and in vitro skin permeation profile formulation ET3 containing 30 mg/ml of chitosan was found to be the best and chosen for further studies. Optimized formulation was subjected to in vivo pharmacokinetic analysis in rats using ELISA.Results: Stability profile of patch formulation ET3 depicted stability up to 3 mo. One week skin irritation evaluation in rats indicated that formulation ET3 was nonirritating. Combination transdermal patch across rat skin showed a maximum release of 92.936 and 95.03 % in 60 h with a flux of 2.088 and 21.398 µg/cm2h for ethinylestradiol and testosterone respectively.Conclusion: The net result of this study is the formulation of a stable, non-irritating transdermal patch of ethinylestradiol and testosterone, with good bioavailability and can be used as Estrogen Replacement Therapy (ERT) in postmenopausal women.

scholarly journals Enhancing effect of modified beta-cyclodextrins on in vitro skin permeation of estradiol

2007 ◽  
Vol 43 (1) ◽  
pp. 111-120 ◽  
Author(s):  
Daniel De Paula ◽  
Dionéia Camilo Rodrigues Oliveira ◽  
Antônio Cláudio Tedesco ◽  
Maria Vitória Lopes Badra Bentley
Keyword(s):  
Skin Permeation ◽  
Enhancing Effect ◽  
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.

scholarly journals Development of Budesonide Loaded Biopolymer Based Dry Powder Inhaler: Optimization, In Vitro Deposition, and Cytotoxicity Study

2014 ◽  
Vol 2014 ◽  
pp. 1-12 ◽  
Author(s):  
Ashwin J. Mali ◽  
Atmaram P. Pawar ◽  
Ravindra N. Purohit
Keyword(s):  
Side Effects ◽  
Active Site ◽  
Lung Diseases ◽  
Dry Powder Inhaler ◽  
Deposition Efficiency ◽  
Therapeutic Delivery ◽  
Drug Molecules ◽  
Systemic Side Effects ◽  
The Subject

The progress in the development of DPI technology has boosted the use of sensitive drug molecules for lung diseases. However, delivery of these molecules from conventional DPI to the active site still poses a challenge with respect to deposition efficiency in the lung. At same time, serious systemic side effects of drugs have become a cause for concern. The developed budesonide loaded biopolymer based controlled release DPI had shown maximum in vitro lung deposition with least toxicity. The subject of present study, lactose-free budesonide loaded biopolymer based DPI, further corroborates the great potential of antiasthmatic drugs. This technology is expected to revolutionize the approaches towards enhanced therapeutic delivery of prospective drugs.

scholarly journals Albumin-Albumin/Lactosylated Core-Shell Nanoparticles: Therapy to Treat Hepatocellular Carcinoma for Controlled Delivery of Doxorubicin

Molecules ◽  
2020 ◽  
Vol 25 (22) ◽  
pp. 5432
Author(s):  
Nayelli Guadalupe Teran-Saavedra ◽  
Jose Andrei Sarabia-Sainz ◽  
Enrique Fernando Velázquez-Contreras ◽  
Gabriela Ramos-Clamont Montfort ◽  
Martín Pedroza-Montero ◽  
...  
Keyword(s):  
Hepatocellular Carcinoma ◽  
Side Effects ◽  
Hepg2 Cells ◽  
Core Shell ◽  
Shell Nanoparticles ◽  
Human Liver Cancer ◽  
Systemic Side Effects ◽  
Human Liver Cancer Cells ◽  
Core Shell Nanoparticles

Doxorubicin (Dox) is the most widely used chemotherapeutic agent and is considered a highly powerful and broad-spectrum for cancer treatment. However, its application is compromised by the cumulative side effect of dose-dependent cardiotoxicity. Because of this, targeted drug delivery systems (DDS) are currently being explored in an attempt to reduce Dox systemic side-effects. In this study, DDS targeting hepatocellular carcinoma (HCC) has been designed, specifically to the asialoglycoprotein receptor (ASGPR). Dox-loaded albumin-albumin/lactosylated (core-shell) nanoparticles (tBSA/BSALac NPs) with low (LC) and high (HC) crosslink using glutaraldehyde were synthesized. Nanoparticles presented spherical shapes with a size distribution of 257 ± 14 nm and 254 ± 14 nm, as well as an estimated surface charge of −28.0 ± 0.1 mV and −26.0 ± 0.2 mV, respectively. The encapsulation efficiency of Dox for the two types of nanoparticles was higher than 80%. The in vitro drug release results showed a sustained and controlled release profile. Additionally, the nanoparticles were revealed to be biocompatible with red blood cells (RBCs) and human liver cancer cells (HepG2 cells). In cytotoxicity assays, Dox-loaded nanoparticles decrease cell viability more efficiently than free Dox. Specific biorecognition assays confirmed the interaction between nanoparticles and HepG2 cells, especially with ASGPRs. Both types of nanoparticles may be possible DDS specifically targeting HCC, thus reducing side effects, mainly cardiotoxicity. Therefore, improving the quality of life from patients during chemotherapy.

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