A pre-formulation strategy for the liposome encapsulation of new thioctic acid conjugates for enhanced chemical stability and use as an efficient drug carrier for MPO-mediated atherosclerotic CVD treatment

2020 ◽  
Vol 44 (7) ◽  
pp. 2755-2767
Author(s):  
Premkumar Jayaraj ◽  
Gopal Venkatesh Shavi ◽  
Ananda Kumar Srinivasan ◽  
Ramesh Raghavendra ◽  
Akella Sivaramakrishna ◽  
...  
Keyword(s):  
Chemical Stability ◽  
Drug Carrier ◽  
Thioctic Acid ◽  
Liposome Encapsulation ◽  
Chemical Approach

Lipoyl-apocynin and lipoyl-sesamol are bio-active conjugates of thioctic acid, synthesized using a benign chemical approach via the combination of thioctic acid and the powerful bio-phytonutrients, apocynin and sesamol, respectively.

Chemical stability of N-trifluoroacetyldoxorubicin-14-valerate (AD-32) in aqueous media and after liposome encapsulation

1989 ◽  
Vol 56 (2) ◽  
pp. 103-109 ◽  
Author(s):  
O. Bekers ◽  
J.H. Beijnen ◽  
G. Storm ◽  
A. Bult ◽  
W.J.M. Underberg
Keyword(s):  
Chemical Stability ◽  
Aqueous Media ◽  
Liposome Encapsulation

Thrombolytic Treatment with Tissue-type Plasminogen Activator (t-PA) Containing Liposomes in Rabbits: a Comparison with Free t-PA

1995 ◽  
Vol 73 (03) ◽  
pp. 488-494 ◽  
Author(s):  
J L M Heeremans ◽  
R Prevost ◽  
M E A Bekkers ◽  
P Los ◽  
J J Emeis ◽  
...  
Keyword(s):  
Plasminogen Activator ◽  
Therapeutic Index ◽  
Tissue Type ◽  
Jugular Vein Thrombosis ◽  
Thrombolytic Activity ◽  
Tissue Type Plasminogen Activator ◽  
Liposome Encapsulation ◽  
Thrombosis Model ◽  
Lysis Activity ◽  
Type Plasminogen Activator

SummaryIn this study, we aimed at improving the therapeutic index of tissue- type Plasminogen Activator (t-PA) as thrombolytic agent in the treatment of myocardial infarction. Liposome-encapsulated t-PA was tested in a rabbit jugular vein thrombosis model: administration of free t-PA (t-PA) as a bolus injection in the ear vein was compared to a similar administration of liposomal t-PA (t-PA-lip), liposomal t-PA in plasminogen-coated liposomes (Plg-t-PA-lip), a mixture of free t-PA and empty liposomes (t-PA+empty lip) and a saline-blank (blank) in terms of thrombolytic activity and side effects.Liposomal t-PA (t-PA-lip/Plg-t-PA-lip) showed a significantly better thrombolysis efficiency than equimolar doses of free t-PA (t-PA/ t-PA+ empty lip): about 0.24 mg/kg of liposomal t-PA practically equalled the lysis-activity of a dose of free t-PA of 1.0 mg/kg (t-PAlmg/kg). On the other hand, liposome encapsulation did not affect the systemic activation of alpha2-antiplasmin and plasminogen by t-PA.We conclude that for this model an improvement in thrombolytic efficacy of t-PA is achieved by liposome encapsulation of t-PA. As t-PA-lip and Plg-t-PA-lip -treatment induced similar results, targeting of liposomal t-PA by coupled glu-Plg remains a topic to be optimized in future studies.

Solubility Enhancement of Poorly Soluble Drug Simvastatin by Solid Dispersion Technique

2016 ◽  
Vol 2 (2) ◽  
pp. 91-95
Author(s):  
Neelima Rani T ◽  
Pavani A ◽  
Sobhita Rani P ◽  
Srilakshmi N
Keyword(s):  
Dissolution Rate ◽  
Drug Carrier ◽  
Solid Dispersions ◽  
Aqueous Solubility ◽  
Onset Of Action ◽  
Kneading Method ◽  
Wetting Property ◽  
Poorly Soluble ◽  
Dispersion Technique ◽  
Low Solubility

This study aims to formulate solid dispersions (SDs) of Simvastatin (SIM) to improve the aqueous solubility, dissolution rate and to facilitate faster onset of action. Simvastatin is a BCS class II drug having low solubility & therefore low oral bioavailability. In the present study, SDs of simvastatin different drug-carrier ratios were prepared by kneading method. The results showed that simvastatin solubility & dissolution rate enhanced with polymer SSG in the ratio 1:7 due to increase in wetting property or possibly may be due to change in crystallinity of the drug.

The Role of Stent Design and Polymers in Safety Outcomes – A Review

2012 ◽  
Vol 8 (1) ◽  
pp. 63
Author(s):  
Carlo Zivelonghi ◽  
Giulia Geremia ◽  
Michele Pighi ◽  
Flavio Ribichini ◽  
◽  
...  
Keyword(s):  
Clinical Performance ◽  
Drug Carrier ◽  
Chemical Properties ◽  
Vascular Wall ◽  
Radial Force ◽  
Vascular Trauma ◽  
Polymer Composition ◽  
Drug Eluting Stent ◽  
Stent Design ◽  
Drug Elution

Each component of a drug-eluting stent (DES) contributes to the safety of the device. Continuous efforts are being dedicated to the search of the optimal compromise between facility of use, safety and long-term efficacy. Shorter balloons reduce the vascular trauma beyond the stent struts; the metallic composition of the stent platform and the platform itself interact with the vascular wall in a long-lasting equilibrium between radial force, vessel patency and reparative cellular regrowth. The modality of drug elution is largely regulated by the chosen drug carrier, rather than by the chemical properties of the drug itself. Drug elution can be accomplished by permanent polymers that remain in the vessel wall forever, by biodegradable polymers that leave the naked metallic structure behind after their complete absorption, or even by direct release of the drug from stent reservoirs. The clinical performance of DESs has been exhaustively assessed in a large number of studies that have showed rapid and continuous improvements, from the first-generation DESs to the latest devices, based on substantial changes in stent design and polymer composition.

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