Faculty Opinions recommendation of l-Serine-modified polyamidoamine dendrimer as a highly potent renal targeting drug carrier.

2018 ◽  
Author(s):  
Donald A Tomalia
Keyword(s):  
Drug Carrier ◽  
Polyamidoamine Dendrimer

scholarly journals l-Serine–modified polyamidoamine dendrimer as a highly potent renal targeting drug carrier

2018 ◽  
Vol 115 (41) ◽  
pp. 10511-10516 ◽  
Author(s):  
Satoru Matsuura ◽  
Hidemasa Katsumi ◽  
Hiroe Suzuki ◽  
Natsuko Hirai ◽  
Hidetaka Hayashi ◽  
...  
Keyword(s):  
Computed Tomography ◽  
Single Photon ◽  
Kidney Diseases ◽  
Drug Carrier ◽  
Photon Emission ◽  
Fluorescein Isothiocyanate ◽  
Drug Carriers ◽  
Ace Inhibition ◽  
Emission Computed Tomography ◽  
Polyamidoamine Dendrimer

Effective delivery of drug carriers selectively to the kidney is challenging because of their uptake by the reticuloendothelial system in the liver and spleen, which limits effective treatment of kidney diseases and results in side effects. To address this issue, we synthesized l-serine (Ser)–modified polyamidoamine dendrimer (PAMAM) as a potent renal targeting drug carrier. Approximately 82% of the dose was accumulated in the kidney at 3 h after i.v. injection of 111In-labeled Ser-PAMAM in mice, while i.v. injection of 111In-labeled unmodified PAMAM, l-threonine modified PAMAM, and l-tyrosine modified PAMAM resulted in kidney accumulations of 28%, 35%, and 31%, respectively. Single-photon emission computed tomography/computed tomography (SPECT/CT) images also indicated that 111In-labeled Ser-PAMAM specifically accumulated in the kidneys. An intrakidney distribution study showed that fluorescein isothiocyanate-labeled Ser-PAMAM accumulated predominantly in renal proximal tubules. Results of a cellular uptake study of Ser-PAMAM in LLC-PK1 cells in the presence of inhibitors [genistein, 5-(N-ethyl-N-isopropyl)amiloride, and lysozyme] revealed that caveolae-mediated endocytosis, micropinocytosis, and megalin were associated with the renal accumulation of Ser-PAMAM. The efficient renal distribution and angiotensin-converting enzyme (ACE) inhibition effect of captopril (CAP), an ACE inhibitor, was observed after i.v. injection of the Ser-PAMAM-CAP conjugate. These findings indicate that Ser-PAMAM is a promising renal targeting drug carrier for the treatment of kidney diseases. Thus, the results of this study demonstrate efficient renal targeting of a drug carrier via Ser modification.

Studying the dynamic mechanism of transporting a single drug carrier-polyamidoamine dendrimer through cell membranes by force tracing

Nanoscale ◽  
2016 ◽  
Vol 8 (42) ◽  
pp. 18027-18031 ◽  
Author(s):  
Boyu Yang ◽  
Haijiao Xu ◽  
Shaowen Wang ◽  
Mingjun Cai ◽  
Yan Shi ◽  
...  
Keyword(s):  
Cell Membranes ◽  
Drug Carrier ◽  
Dynamic Mechanism ◽  
Polyamidoamine Dendrimer ◽  
Single Drug

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.

Chitosan-based Polymer Matrix for Pharmaceutical Excipients and Drug Delivery

2019 ◽  
Vol 26 (14) ◽  
pp. 2502-2513 ◽  
Author(s):  
Md. Iqbal Hassan Khan ◽  
Xingye An ◽  
Lei Dai ◽  
Hailong Li ◽  
Avik Khan ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Drug Carrier ◽  
Drug Loading ◽  
Delivery Systems ◽  
Cancer Drug ◽  
Release Mechanism ◽  
Innovative Drug ◽  
Pharmaceutical Excipients ◽  
Weight Variation

The development of innovative drug delivery systems, versatile to different drug characteristics with better effectiveness and safety, has always been in high demand. Chitosan, an aminopolysaccharide, derived from natural chitin biomass, has received much attention as one of the emerging pharmaceutical excipients and drug delivery entities. Chitosan and its derivatives can be used for direct compression tablets, as disintegrant for controlled release or for improving dissolution. Chitosan has been reported for use in drug delivery system to produce drugs with enhanced muco-adhesiveness, permeation, absorption and bioavailability. Due to filmogenic and ionic properties of chitosan and its derivative(s), drug release mechanism using microsphere technology in hydrogel formulation is particularly relevant to pharmaceutical product development. This review highlights the suitability and future of chitosan in drug delivery with special attention to drug loading and release from chitosan based hydrogels. Extensive studies on the favorable non-toxicity, biocompatibility, biodegradability, solubility and molecular weight variation have made this polymer an attractive candidate for developing novel drug delivery systems including various advanced therapeutic applications such as gene delivery, DNA based drugs, organ specific drug carrier, cancer drug carrier, etc.

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