scholarly journals A twofold strategy for the protection of therapeutic peptides by attachment to the protease-resistant and fusogenic protein, saposin C

2020 ◽  
Author(s):  
Suzanne I. Sandin ◽  
Christopher J. Randolph ◽  
Eva de Alba
Keyword(s):  
Drug Delivery ◽  
Half Life ◽  
Liposome Membrane ◽  
Saposin C ◽  
Additional Protection ◽  
Therapeutic Peptides ◽  
Covalently Linked ◽  
The Individual ◽  
Endocytic Pathways

ABSTRACTA great challenge of therapeutic peptides (biologics) is their short half-life. However, biologics can be protected by encapsulation in liposomes used as drug-delivery platforms. Liposomes are typically incorporated into cells by endocytic pathways, which eventually expose therapeutics to favorable proteolytic conditions. To enhance biologics protection, we report the design and characterization of a liposome-protein chimera combining the liposome fusogenic properties of peripheral-membrane protein saposin C, covalently linked to a proapoptotic peptide (the active domain of Bcl-2 protein PUMA). We show by NMR that the saposin C component of the chimera is capable of binding liposomes and that the peptide binds prosurvival Bcl-xL, thus following known PUMA’s mechanism to induce cell death. These results indicate that the function of the individual components is preserved in the chimera. Our results point to a promising twofold strategy for drug delivery to; 1) avoid endocytosis by promoting liposome-membrane fusion, 2) provide additional protection by attachment to a stable, protease-resistant protein, which is a well-known method commonly used to prolong biologics half-life.

Development and in vivo characterization of a novel peptide drug delivery system providing extended plasma half life

2012 ◽  
Vol 157 (3) ◽  
pp. 375-382 ◽  
Author(s):  
Gul Shahnaz ◽  
Javed Iqbal ◽  
Deni Rahmat ◽  
Glen Perera ◽  
Flavia Laffleur ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Half Life ◽  
Peptide Drug ◽  
Extended Plasma ◽  
In Vivo Characterization ◽  
Plasma Half Life

Biopolymers with Medical Applications Optimized method for obtaining chitosan-based delivery systems

2018 ◽  
Vol 69 (7) ◽  
pp. 1756-1759 ◽  
Author(s):  
Luminita Confederat ◽  
Iuliana Motrescu ◽  
Sandra Constantin ◽  
Florentina Lupascu ◽  
Lenuta Profire
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Average Diameter ◽  
Delivery Systems ◽  
Cross Linking ◽  
Low Molecular Weight ◽  
Polymeric Systems ◽  
Chitosan Microparticles ◽  
Degree Of Swelling

The aim of this study was to optimize the method used for obtaining microparticles based on chitosan � a biocompatible, biodegradable, and nontoxic polymer, and to characterize the developed systems. Chitosan microparticles, as drug delivery systems were obtained by inotropic gelation method using pentasodiumtripolyphosphate (TPP) as cross-linking agent. Chitosan with low molecular weight (CSLMW) in concentration which ranged between 0.5 and 5 %, was used while the concentration of cross-linking agent ranged between 1 and 5%. The characterization of the microparticles in terms of shape, uniformity and adhesion was performed in solution and dried state. The size of the microparticles and the degree of swelling were also determined. The structure and the morphology of the developed polymeric systems were analyzed by Fourier transform infrared spectroscopy (FTIR) and scanning electron microscopy (SEM).The average diameter of the chitosan microparticles was around 522 �m. The most stable microparticles were obtained using CSLMW 1% and TPP 2% or CSLMW 0.75%and TPP 1%. The micropaticles were spherical, uniform and without flattening. Using CSLMW in concentration of 0.5 % poorly cross-linked and crushed microparticles have been obtained at all TPP concentrations. By optimization of the method, stable chitosan-based micropaticles were obtained which will be used to develop controlled release systems for drug delivery.

Hydrogel-clay Nanocomposites as Carriers for Controlled Release

2020 ◽  
Vol 27 (6) ◽  
pp. 919-954 ◽  
Author(s):  
Raluca Ianchis ◽  
Claudia Mihaela Ninciuleanu ◽  
Ioana Catalina Gifu ◽  
Elvira Alexandrescu ◽  
Cristina Lavinia Nistor ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Controlled Release ◽  
Hybrid Materials ◽  
Pharmaceutical Formulations ◽  
Tree Of Life ◽  
Present Review ◽  
Clay Nanocomposites ◽  
Delivery Platform ◽  
Complex Hybrid

The present review aims to summarize the research efforts undertaken in the last few years in the development and testing of hydrogel-clay nanocomposites proposed as carriers for controlled release of diverse drugs. Their advantages, disadvantages and different compositions of polymers/biopolymers with diverse types of clays, as well as their interactions are discussed. Illustrative examples of studies regarding hydrogel-clay nanocomposites are detailed in order to underline the progressive researches on hydrogel-clay-drug pharmaceutical formulations able to respond to a series of demands for the most diverse applications. Brief descriptions of the different techniques used for the characterization of the obtained complex hybrid materials such as: swelling, TGA, DSC, FTIR, XRD, mechanical, SEM, TEM and biology tests, are also included. Enlightened by the presented data, we can suppose that hydrogel-clay nanocomposites will still be a challenging subject of global assiduous researches. We can dare to dream to an efficient drug delivery platform for the treatment of multiple affection concomitantly, these being undoubtedly like ”a tree of life” bearing different kinds of fruits and leaves proper for human healing.

Separation and Characterization of Standard Propoxyphene Diastereomers and Their Determination in Pharmaceutical and Illicit Preparations

1981 ◽  
Vol 64 (4) ◽  
pp. 875-883
Author(s):  
Shiv K Soni ◽  
Daniel Van Gelder
Keyword(s):  
High Pressure ◽  
Optical Isomers ◽  
Gold Chloride ◽  
Melting Points ◽  
Eutectic Melting ◽  
Racemic Mixtures ◽  
The Individual ◽  
Isomeric Mixtures ◽  
Asymmetric Carbon

Abstract Due to the existence of 2 asymmetric carbon atoms in: the propoxyphene molecule, there are 4 diastereomers: alpha dextro, alpha levo, beta dextro, and beta levo. Only α-d-propoxyphene is included under the federal Controlled Substances Act. Baseline separations of propoxyphene from various incipients (aspirin, caffeine, phenacetin, and acetaminophen) present in pharmaceutical and illicit preparations, and between the alpha and beta diastereomers, were achieved by high pressure liquid chromatography. The column eluant was collected and propoxyphene was extracted. The optical isomers were differentiated and characterized by melting points and by chemical microcrystalline tests. Using hot stage thermomicroscopy, the eutectic melting points of binary isomeric mixtures of propoxyphene bases and salts were found to be depressed about 10° and 15-30°C, respectively, below the individual isomer melting points. The characteristic microcrystals formed with the alpha racemic mixtures by using a glycerin-aqueous gold chloride reagent were not produced by the beta racemic mixtures.

Sign in / Sign up

Export Citation Format

Share Document