Hybrid polymeric nanoparticles with high zoledronic acid payload and proton sponge-triggered rapid drug release for anticancer applications

2020 ◽  
Vol 116 ◽  
pp. 111277 ◽  
Author(s):  
Min-Cong Xiao ◽  
Ya-Hsuan Chou ◽  
Yu-Ning Hung ◽  
Shang-Hsiu Hu ◽  
Wen-Hsuan Chiang
Polymers ◽  
2021 ◽  
Vol 13 (13) ◽  
pp. 2180
Author(s):  
Sana Javaid ◽  
Nasir M. Ahmad ◽  
Azhar Mahmood ◽  
Habib Nasir ◽  
Mudassir Iqbal ◽  
...  

The objective of the present study was to achieve the successful encapsulation of a therapeutic agent to achieve antifouling functionality regarding biomedical applications. Considering nanotechnology, drug-loaded polycaprolactone (PCL)-based nanoparticles were prepared using a nano-precipitation technique by optimizing various process parameters. The resultant nano-formulations were investigated for in vitro drug release and antifouling applications. The prepared particles were characterized in terms of surface morphology and surface properties. Optimized blank and drug-loaded nanoparticles had an average size of 200 nm and 216 nm, respectively, with associated charges of −16.8 mV and −11.2 mV. Studies of the in vitro release of drug were carried out, which showed sustained release at two different pH, 5.5 and 7.4 Antifouling activity was observed against two bacterial strains, Gram-positive Staphylococcus aureus and Gram-negative Escherichia coli. The zone of inhibition of the optimized polymeric drug-loaded nanoparticle F-25 against both strains were compared with the pure drug. The gradual pH-responsive release of antibiotics from the biodegradable polymeric nanoparticles could significantly increase the efficiency and pharmacokinetics of the drug as compared to the pure drug. The acquired data significantly noted that the resultant nano-encapsulation of antifouling functionality could be a promising candidate for topical drug delivery systems and skin applications.


2014 ◽  
Vol 50 (4) ◽  
pp. 869-876 ◽  
Author(s):  
Neha Gulati ◽  
Upendra Nagaich ◽  
Shubhini Saraf

The objective of the research was to formulate and evaluate selegiline hydrochloride loaded chitosan nanoparticles for the Parkinson's therapy in order to improve its therapeutic effect and reducing dosing frequency. Taguchi method of design of experiments (L9 orthogonal array) was used to get optimized formulation. The selegiline hydrochloride loaded chitosan nanoparticles (SHPs) were prepared by ionic gelation of chitosan with tripolyphosphate anions (TPP) and tween 80 as surfactant. The SHPs had a mean size of (303.39 ± 2.01) nm, a zeta potential of +32.50mV, and entrapment efficiency of SHPs was 86.200 ± 1.38%. The in vitro drug release of SHPs was evaluated in phosphate buffer saline (pH 5.5) using goat nasal mucosa and found to be 82.529% ± 1.308 up to 28 h. Release kinetics studies showed that the release of drug from nanoparticles was anomalous (non-fickian) diffusion indicating the drug release is controlled by more than one process i.e. superposition of both phenomenon, the diffusion controlled as well as swelling controlled release. SHPs showed good stability results as found during stability studies at different temperatures as mentioned in ICH guidelines. The results revealed that selegiline hydrochloride loaded chitosan nanoparticles are most suitable mode of delivery of drug for promising therapeutic action.


Author(s):  
MONOWAR HUSSAIN ◽  
ANUPAM SARMA ◽  
SHEIKH SOFIUR RAHMAN ◽  
ABDUL MATIN SIDDIQUE ◽  
TANUKU PAVANI EESWARI

Objective: Tuberculosis (TB) is an infectious bacterial disease caused by Mycobacterium tuberculosis which most commonly affects the lungs. TB has the highest mortality rate than any other infectious disease occurs worldwide. The main objective of the present investigation was to develop polymeric nanoparticles based drug delivery system to sustain the ethambutol (ETB) release by reducing the dose frequency. Methods: The Preformulation studies of drug ETB were done by physical characterization, melting point determination, and UV spectrophotometric analysis. The ETB loaded nanoparticles were prepared by double-emulsion (W/O/W) solvent evaporation/diffusion technique. The prepared polymeric nanoparticles were evaluated for particle size, polydispersity index, zeta potential, drug entrapment efficiency, drug loading, drug-polymer compatibility study, surface morphology, in vitro drug release, and release kinetics. Results: Based on the result obtained from the prepared formulations, F11 showed the best result and was selected as the optimized formulation. Optimized batch (F11) showed better entrapment efficiency (73.3%), good drug loading capacity (13.21%), optimum particle size (136.1 nm), and zeta potential (25.2 mV) with % cumulative drug release of 79.08% at the end of 24 h. Conclusion: These results attributed that developed polymeric nanoparticles could be effective in sustaining the ETB release over 24 h. Moreover, the developed nanoparticles could be an alternate method for ETB delivery with a prolonged drug release profile and a better therapeutic effect can be achieved for the treatment of tuberculosis.


2006 ◽  
Vol 323 (1-2) ◽  
pp. 146-152 ◽  
Author(s):  
Surendra Nimesh ◽  
Romila Manchanda ◽  
Rupesh Kumar ◽  
Amit Saxena ◽  
Preeti Chaudhary ◽  
...  

2018 ◽  
Vol 3 (4) ◽  
pp. 397-407 ◽  
Author(s):  
Haisheng He ◽  
Sifan Jiang ◽  
Yunchang Xie ◽  
Yi Lu ◽  
Jianping Qi ◽  
...  

Fast drug release leads to divergent kinetics of paclitaxel and mPEG-PCL nanoparticles, justifying an updated understanding of long circulation.


2020 ◽  
Author(s):  
Sheyda Shakiba ◽  
Carlos E. Astete ◽  
Rafael Cueto ◽  
Debora F. Rodrigues ◽  
Cristina M. Sabliov ◽  
...  

Polymeric nanoparticles (NPs) are typically designed to enhance the efficiency of drug delivery by controlling the drug release rate. Hence, it is critical to obtain an accurate drug release profile. This study presents the first application of asymmetric flow field-flow fractionation (AF4) with fluorescence detection (FLD) to characterize release profiles of fluorescent drugs from polymeric NPs, specifically poly lactic-co-glycolic acid NPs loaded with enrofloxacin (PLGA-Enro NPs). In contrast to traditional release measurements requiring separation of entrapped and dissolved drugs (typically by dialysis) prior to quantification, AF4-FLD provides in situ purification of the NPs from unincorporated drugs, along with direct measurement of the entrapped drug. Size distributions and shape factors are simultaneously obtained by online dynamic and multi-angle light scattering detectors. The AF4-FLD and dialysis approaches were compared to evaluate drug release from PLGA-Enro NPs containing a high proportion (≈ 88%) of unincorporated (burst release) drug at three different temperatures spanning the glass transition temperature (30 °C for PLGA-Enro NPs). The AF4-FLD analysis was able to identify size-dependent release rates across the entire continuous NP size distribution, with smaller NPs showing faster release. The AF4-FLD method also clearly captured the expected temperature dependence of the drug release (from almost no release at 20 °C to rapid release at 37 °C). In contrast, dialysis was not able to distinguish these differences in the extent or rate of release of the entrapped drug because of interferences from the burst release background, as well as the dialysis lag time. A mechanistic diffusion model that integrates data from both AF4-FLD and dialysis further supported the advantages of AF4-FLD to capture the true release rate of entrapped drug and avoid artifacts observed in dialysis. Overall, this study demonstrates the novel application and unique advantages of AF4-FLD methods to obtain direct, size-resolved release profiles of fluorescent drugs from polymeric NPs.


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