scholarly journals The Synthesis of Peptide-Conjugated Poly(2-Ethyl-2-Oxazoline)-bpoly(L-Lactide) (PEtOx-B-PLA) Polymeric Systems Through the Combination of Controlled Polymerization Techniques and Click Reactions

Author(s):  
Umut Ugur Ozkose ◽  
Sevgi Gulyuz ◽  
Melek Parlak Khalily ◽  
Salih Ozcubukcu ◽  
Asuman Bozkır ◽  
...  

To optimize the therapeutic effect of pharmaceutical agents, drug delivery systems tailored from FDA-approved polymers like poly(L-lactide) (PLA) is an effective strategy. Because of their hydrophobic character, these systems greatly suffer from reduced circulation time thus, amphiphilic block copolymers became favourable to overcome this limitation. Of them, poly(oxazoline)-b-poly(L-lactide) are of choice as poly(oxazoline) (PEtOx) is compatibile, biodegradable, while exhibiting minimum cytotoxicity. To tailor selective drug targeting drug delivery systems, whereby their selectivity for tumour tissues is maximised, these polymers should be decorated with so-called tumour-homing agents, such as antibodies, peptides and so forth. To this respect, we designed a new block copolymer, allyl-poly(2-ethyl-2-oxazoline)-b-poly(L-lactide) allyl-(PEtOx-b-PLA) and its subsequent conjugation to tumour-homing peptides, peptide-18 and peptide-563 at the terminal position. In this manuscript, we report our synthetic route to obtain this building block and its conjugation to tumour-homing agents.

2020 ◽  
Author(s):  
Umut Ugur Ozkose ◽  
Sevgi Gulyuz ◽  
Melek Parlak Khalily ◽  
Salih Ozcubukcu ◽  
Asuman Bozkır ◽  
...  

To optimize the therapeutic effect of pharmaceutical agents, drug delivery systems tailored from FDA-approved polymers like poly(L-lactide) (PLA) is an effective strategy. Because of their hydrophobic character, these systems greatly suffer from reduced circulation time thus, amphiphilic block copolymers became favourable to overcome this limitation. Of them, poly(oxazoline)-b-poly(L-lactide) are of choice as poly(oxazoline) (PEtOx) is compatibile, biodegradable, while exhibiting minimum cytotoxicity. To tailor selective drug targeting drug delivery systems, whereby their selectivity for tumour tissues is maximised, these polymers should be decorated with so-called tumour-homing agents, such as antibodies, peptides and so forth. To this respect, we designed a new block copolymer, allyl-poly(2-ethyl-2-oxazoline)-b-poly(L-lactide) allyl-(PEtOx-b-PLA) and its subsequent conjugation to tumour-homing peptides, peptide-18 and peptide-563 at the terminal position. In this manuscript, we report our synthetic route to obtain this building block and its conjugation to tumour-homing agents.


2018 ◽  
Vol 69 (7) ◽  
pp. 1756-1759 ◽  
Author(s):  
Luminita Confederat ◽  
Iuliana Motrescu ◽  
Sandra Constantin ◽  
Florentina Lupascu ◽  
Lenuta Profire

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.


2020 ◽  
Vol 11 (2) ◽  
pp. 2505-2518
Author(s):  
Sindhuja Devaraj ◽  
Ganesh GNK

Nanoparticulate drug delivery system are the rapidly developing system, and nanoparticles are present in the size range of 1-100nm. Nanoparticles composed of various thermal, electrical, and optical property. Nanoparticles offers the potential advantages over the traditional dosage forms it is ascribable to the properties of nanoparticles. Nanoparticulate drug delivery system ensures the site-specific delivery of a drug(Targeting drug delivery) and aids in improving the efficacy of the new as well as old drugs and has the potential in crossing the various physiological barriers and also improves the therapeutic index of the drugs and increases the patient compliance. The objectives of this review is to classify the nanoparticles based on the different groups, surface properties of nanoparticles, describe the strategies of drug targeting, the necessity of nanoparticles their general method of preparation, different methods used in characterization, self- assembly and mechanism of drug release in a systemic manner. The potential advantages and limitations of various nanoparticulate drug delivery systems are also discussed elaborately.


Author(s):  
SWAMINATHAN V. ◽  
VAIYANA RAJESH C.

The objective of the review is to present the contemporary approaches involved in colonic drug targeting for the therapy of inflammatory bowel disease (IBD). The adverse reactions and side-effects of the conventional drug delivery systems are largely on account of the systemic absorption of the drugs from the small intestine. Moreover, in current drug delivery systems, the drug has to be frequently administered and also in larger doses which greatly reduces patient compliance. Various approaches which are being described here mainly target the colonic region specifically for improved therapy of IBD, by increasing localization and accessibility of the drug to the target site. Also, these approaches will result in the reduction of dose and minimization of adverse effects combined with the use of conventional drug delivery systems.


2018 ◽  
Vol 18 (8) ◽  
pp. 792-806 ◽  
Author(s):  
Urvashi Aggarwal ◽  
Amit Kumar Goyal ◽  
Goutam Rath

Cervical cancer is the second most common cancer in women. Standard treatment options available for cervical cancer include chemotherapy, surgery and radiation therapy associated with their own side effects and toxicities. Tumor-targeted delivery of anticancer drugs is perhaps one of the most appropriate strategies to achieve optimal outcomes from the treatment and improve the quality of life. Recently nanocarriers based drug delivery systems owing to their unique properties have been extensively investigated for anticancer drug delivery. In addition to that addressing the anatomical significance of cervical cancer, various local drug delivery strategies for the cancer treatment are introduced like: gels, nanoparticles, polymeric films, rods and wafers, lipid based nanocarrier. Localized drug delivery systems allow passive drug targeting results in high drug concentration at the target site. Further they can be tailor made to achieve both sustained and controlled release behavior, substantially improving therapeutic outcomes and minimizing side effects. This review summarizes the meaningful advances in drug delivery strategies to treat cervical cancer.


Author(s):  
Vinod K R ◽  
Sridhar D ◽  
Sandhya S ◽  
Banji D ◽  
Rohit Reddy T

There is a renewed focus on developing formulation strategies for the regional drug targeting. Magnetic drug targeting provides an innovative approach that may include two and three dimensional arrays of magnetic drug delivery systems. Applications of magnetic microsphere-based drug delivery include chemotherapy, arthritis, gene, and cell transplantation therapy. This article describes different formulation approaches, routes of administration, and mechanisms of magnetic-based drug targeting. Magnetic materials have to be synthesized before considering the formulation development. Although the preparation evaluation of magnetic drug delivery is comparable with conventional microspheres and nanoparticles, characterization of magnetic properties of the final formulation is very essential for success of this approach.  In vivo evaluation studies include tumor targeting in animals, histological evaluation using MRI and course of the magnetic drug delivery system by image mapping using suitable biological markers.


2020 ◽  
Author(s):  
Tae Joon Kwak ◽  
Huihun Jung ◽  
Benjamin D Allen ◽  
Melik C Demirel ◽  
Woo-Jin Chang

AbstractRecently, insoluble protein particles have been increasingly investigated for artificial drug delivery systems due to their favorable properties, including programmability for active drug targeting of diseases as well as their biocompatibility and biodegradability after administration. One of the biggest challenges is selectively collecting monodisperse particles in desirable morphologies and sizes to enable consistent levels and rates of drug loading and release. Therefore, technology that allows sorting of protein particles with respect to size and morphology will enhance the design and production of next-generation drug delivery materials. Here, we introduce a dielectrophoretic (DEP) separation technique to selectively isolate spherical protein particles from a mixture of randomly shaped particles. We tested this approach by applying it to a mixture of precipitated squid ring teeth inspired tandem repeat protein particles with diverse sizes and morphologies. The DEP trapping system enabled us to isolate specific-sized, spherical protein particles out of this mixture: after separation, the fraction of 2 μm and 4 μm spherical particles was increased from 28.64% of mixture to 80.53% and 74.02% with polydispersity indexes (PDIs) decreased from 0.93 of mixture to 0.19 and 0.09, respectively. The protein particles show high aqueous swelling capability (up to 74% by mass) that could enable delivery of drug solutions. This work is intended to inspire the future development of biocompatible drug-delivery systems.


2019 ◽  
Vol 9 (1-s) ◽  
pp. 377-380
Author(s):  
Zhengwei Zhang

Treatment of tumors with nanoparticles and combined drugs tend to turn effective as it can sustain for a longer time in the recipient’s body and also improve the impact. The conjugates that have proven to have high cytotoxicity are suggested in this report. Pegylation is an advanced drug delivery system that maximizes the immunity of the patient and helps in the correct targeting of the affected cells. Keywords: Tumors, Nanoparticles, Drug targeting


Sign in / Sign up

Export Citation Format

Share Document