Nanomized tumor-microenvironment-active NIR fluorescent prodrug for ensuring synchronous occurrences of drug release and fluorescence tracing

2019 ◽  
Vol 7 (9) ◽  
pp. 1503-1509 ◽  
Author(s):  
Qiang Li ◽  
Jun Cao ◽  
Qi Wang ◽  
Jie Zhang ◽  
Shiqin Zhu ◽  
...  

A nanomized NIR fluorescent prodrug was developed with improved bioavailability and tumor-targeting ability. Nanomized tumor-microenvironment-active NIR DCM-S-GEM/PEG prodrug provides a novel approach to realize long real-time tracking of drug delivery and activation process without systemic toxicity in vivo.


2020 ◽  
Vol 28 (5) ◽  
pp. 538-549 ◽  
Author(s):  
Fatima Akbar Sheikh ◽  
Muhammad Ajaz Hussain ◽  
Muhammad Umer Ashraf ◽  
Muhammad Tahir Haseeb ◽  
Muhammad Farid-ul-Haq


2018 ◽  
Vol 61 (10) ◽  
pp. 1293-1300 ◽  
Author(s):  
Zhiqian Guo ◽  
Yaguang Ma ◽  
Yajing Liu ◽  
Chenxu Yan ◽  
Ping Shi ◽  
...  


Author(s):  
Natalia Feiner-Gracia ◽  
Adrianna Glinkowska Mares ◽  
Marina Buzhor ◽  
Romen Rodriguez-Trujillo ◽  
Josep Samitier ◽  
...  

ABSTRACTThe performance of supramolecular nanocarriers as drug delivery systems depends on their stability in the complex and dynamic biological media. After administration, nanocarriers are challenged by confronting different barriers such as shear stress and proteins present in blood, endothelial wall, extracellular matrix and eventually cancer cell membranes. While early disassembly will result in a premature drug release, extreme stability of the nanocarriers can lead to poor drug release and low efficiency. Therefore, comprehensive understanding of the stability and assembly state of supramolecular carriers in each stage of delivery is a key factor for the rational design of these systems. One of the key challenges is that current 2D in vitro models do not provide exhaustive information, as they do not fully recapitulate the 3D tumor microenvironment. This deficiency of the 2D models complexity is the main reason for the differences observed in vivo when testing the performance of supramolecular nanocarriers. Herein, we present a real-time monitoring study of self-assembled micelles stability and extravasation, combining spectral confocal microscopy and a microfluidic tumor-on-a-chip. The combination of advanced imaging and a reliable organ-on-a-chip model allow us to track micelle disassembly by following the spectral properties of the amphiphiles in space and time during the crucial steps of drug delivery. The spectrally active micelles were introduced under flow and their position and conformation followed during the crossing of barriers by spectral imaging, revealing the interplay between carrier structure, micellar stability and extravasation. Integrating the ability of the micelles to change their fluorescent properties when disassembled, spectral confocal imaging and 3D microfluidic tumor blood vessel-on-a-chip, resulted in the establishment of a robust testing platform, suitable for real-time imaging and evaluation of supramolecular drug delivery carrier’s stability.



Small ◽  
2017 ◽  
Vol 13 (7) ◽  
Author(s):  
Sing Shy Liow ◽  
Qingqing Dou ◽  
Dan Kai ◽  
Zibiao Li ◽  
Sigit Sugiarto ◽  
...  
Keyword(s):  


Author(s):  
YOHEI HAMANAKA ◽  
KOHSUKE GONDA ◽  
KOUICHI SHIRAISHI ◽  
MASAYUKI YOKOYAMA ◽  
MOTOHIRO TAKEDA ◽  
...  


2020 ◽  
Vol 56 (7) ◽  
pp. 1042-1045 ◽  
Author(s):  
Yu-Hui Zhang ◽  
Ying-Ming Zhang ◽  
Xianliang Sheng ◽  
Jie Wang ◽  
Yu Liu

An enzyme-responsive polysaccharide assembly was constructed, which possesses low cytotoxicity, targeted imaging and controlled drug release, while providing a concurrent means for the real-time tracking of drug delivery.



Nanoscale ◽  
2015 ◽  
Vol 7 (10) ◽  
pp. 4451-4460 ◽  
Author(s):  
Jinjian Liu ◽  
Hongzhang Deng ◽  
Qiang Liu ◽  
Liping Chu ◽  
Yumin Zhang ◽  
...  

Integrin-targeted pH-responsive micelles were synthesized with an enhanced drug-loading efficiency, tumor-targeting ability and pH-controlled intracellular drug release for enhanced tumor treatment.



Author(s):  
EL- Assal I. A. ◽  
Retnowati .

Objective of the present investigation was enthused by the possibility to develop solid lipid nanoparticles (SLNs) of hydrophilic drug acyclovir. Also study vitro and vivo drug delivery. Methods: Drug loaded SLNs (ACV-SLNs) were prepared by high pressure homogenization of aqueous surfactant solutions containing the drug-loaded lipids in the melted or in the solid state with formula optimization study (Different lipid concentration, drug loaded, homogenization / stirring speed and compritol 888ATO: drug ratio). ACV - SLN incorporated in cream base. The pH was evaluated and rheological study. Drug release was evaluated and compared with simple cream- drug, ACV – SLN with compritol 888ATO and marketed cream. The potential of SLN as the carrier for dermal delivery was studied. Results: Particle size analysis of SLNs prove small, smooth, spherical shape particle ranged from 150 to 200 nm for unloaded and from 330 to 444 nm for ACV loaded particles. The EE% for optimal formula is 72% with suitable pH for skin application. Rheological behavior is shear thinning and thixotropic. Release study proved controlled drug release for SLNs especially in formula containing compritol88 ATO. Stability study emphasized an insignificant change in SLNs properties over 6 month. In-vivo study showed significantly higher accumulation of ACV in stratum corneum, dermal layer, and receptor compartment compared with blank skin. Conclusion: AVC-loaded SLNs might be beneficial in controlling drug release, stable and improving dermal delivery of antiviral agent(s).



Author(s):  
ShirishaG. Suddala ◽  
S. K. Sahoo ◽  
M. R. Yamsani

Objective: The objective of this research work was to develop and evaluate the floating– pulsatile drug delivery system (FPDDS) of meloxicam intended for Chrono pharmacotherapy of rheumatoid arthritis. Methods: The system consisting of drug containing core, coated with hydrophilic erodible polymer, which is responsible for a lag phase for pulsatile release, top cover buoyant layer was prepared with HPMC K4M and sodium bicarbonate, provides buoyancy to increase retention of the oral dosage form in the stomach. Meloxicam is a COX-2 inhibitor used to treat joint diseases such as osteoarthritis and rheumatoid arthritis. For rheumatoid arthritis Chrono pharmacotherapy has been recommended to ensure that the highest blood levels of the drug coincide with peak pain and stiffness. Result and discussion: The prepared tablets were characterized and found to exhibit satisfactory physico-chemical characteristics. Hence, the main objective of present work is to formulate FPDDS of meloxicam in order to achieve drug release after pre-determined lag phase. Developed formulations were evaluated for in vitro drug release studies, water uptake and erosion studies, floating behaviour and in vivo radiology studies. Results showed that a certain lag time before drug release which was due to the erosion of the hydrophilic erodible polymer. The lag time clearly depends on the type and amount of hydrophilic polymer which was applied on the inner cores. Floating time and floating lag time was controlled by quantity and composition of buoyant layer. In vivo radiology studies point out the capability of the system of longer residence time of the tablets in the gastric region and releasing the drug after a programmed lag time. Conclusion: The optimized formulation of the developed system provided a lag phase while showing the gastroretension followed by pulsatile drug release that would be beneficial for chronotherapy of rheumatoid arthritis and osteoarthritis.



Author(s):  
Anamika Saxena Saxena ◽  
Santosh Kitawat ◽  
Kalpesh Gaur ◽  
Virendra Singh

The main goal of any drug delivery system is to achieve desired concentration of the drug in blood or tissue, which is therapeutically effective and nontoxic for a prolonged period. Various attempts have been made to develop gastroretentive delivery systems such as high density system, swelling, floating system. The recent developments of FDDS including the physiological and formulation variables affecting gastric retention, approaches to design single-unit and multiple-unit floating systems, and their classification and formulation aspects are covered in detail. Gastric emptying is a complex process and makes in vivo performance of the drug delivery systems uncertain. In order to avoid this variability, efforts have been made to increase the retention time of the drug-delivery systems for more than 12 hours. The floating or hydrodynamically controlled drug delivery systems are useful in such application. Background of the research: Diltiazem HCL (DTZ), has short biological half life of 3-4 h, requires rather high frequency of administration. Due to repeated administration there may be chances of patient incompliance and toxicity problems. Objective: The objective of study was to develop sustained release alginate beads of DTZ for reduction in dosing frequency, high bioavailability and better patient compliance. Methodology: Five formulations prepared by using different drug to polymer ratios, were evaluated for relevant parameters and compared. Alginate beads were prepared by ionotropic external gelation technique using CaCl2 as cross linking agent. Prepared beads were evaluated for % yield, entrapment efficiency, swelling index in 0.1N HCL, drug release study and SEM analysis. In order to improve %EE and drug release, LMP and sunflower oil were used as copolymers along with sodium alginate.



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