Improving plasma stability and antitumor effect of gemcitabine via PEGylated liposome prepared by active drug loading

Recently, a drug delivery system with controlled and targeted drug release at the tumor sites emerged as an attractive option for improving anticancer therapeutics. Advanced nanotherapeutics must not be limited to nanoscale, but should find their way to target the solid tumor via direct or indirect way. Pegylation on the surface of liposome helps to become liposome as long-circulating and indirect or passive targeting to tumors. The purpose of this study is to develop and optimize the critical process parameters, which play an important role in the quality pegylated liposome. The design of experiment (DoE) was used to study the impact of critical process variables like hydration temperature, extrusion process temperature, ethanol concentration, drug loading temperature, and drug loading time. Pegylated liposome was prepared using the ethanol injection method. Size reduction was achieved using the extrusion method. Drug encapsulation was achieved by a remote loading method using an ammonium phosphate gradient. A fractional factorial design was chosen for the optimization of process variables. Hydration temperature and extrusion process temperature directly impact on the degradation of lipids used in liposome formation. Higher temperature increases the lipid degradation during the process. The concentration of ethanol during the size reduction process inversely affects the particle size of the liposome. Higher the ethanol content lowers the particle size achieved. The temperature during drug loading process directly affects the degradation of the drug while inversely affect the encapsulation property. Stability study indicates that optimized formulation using DoE approach remains stable. The present research confirms the feasibility of developing and optimizing sterically stabilized liposome using DoE approach.

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Dielectrophoretic separation of randomly shaped protein particles

10.1101/2020.07.23.218438 ◽

2020 ◽

Author(s):

Tae Joon Kwak ◽

Huihun Jung ◽

Benjamin D Allen ◽

Melik C Demirel ◽

Woo-Jin Chang

Keyword(s):

Drug Delivery ◽

Drug Targeting ◽

Drug Delivery Systems ◽

Active Drug ◽

Drug Loading ◽

Delivery Systems ◽

Spherical Particles ◽

Monodisperse Particles ◽

Protein Particles ◽

Size And Morphology

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.

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Four-fold Channel-Nicked Human Ferritin Nanocages for Active Drug Loading and pH-Responsive Drug Release

Angewandte Chemie ◽

10.1002/ange.201800516 ◽

2018 ◽

Vol 130 (11) ◽

pp. 2959-2963

Author(s):

Byungjun Ahn ◽

Seong-Gyu Lee ◽

Hye Ryeon Yoon ◽

Jeong Min Lee ◽

Hyeok Jin Oh ◽

...

Keyword(s):

Drug Release ◽

Active Drug ◽

Drug Loading ◽

Ph Responsive ◽

Human Ferritin

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mPEG5k-b-PLGA2k/PCL3.4k/MCT Mixed Micelles as Carriers of Disulfiram for Improving Plasma Stability and Antitumor Effect in Vivo

Molecular Pharmaceutics ◽

10.1021/acs.molpharmaceut.7b01094 ◽

2018 ◽

Vol 15 (4) ◽

pp. 1556-1564 ◽

Cited By ~ 10

Author(s):

Linlin Miao ◽

Jia Su ◽

Xuezhi Zhuo ◽

Lifeng Luo ◽

Yihan Kong ◽

...

Keyword(s):

Antitumor Effect ◽

Mixed Micelles ◽

Plasma Stability

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Superior antitumor effect of self-assembly supramolecular paclitaxel nanoparticles

RSC Advances ◽

10.1039/d0ra01117g ◽

2020 ◽

Vol 10 (22) ◽

pp. 12999-13005 ◽

Cited By ~ 1

Author(s):

Na Yu ◽

Jun Li ◽

Yuan Zhang ◽

Dan Ding ◽

Xiaolin Li ◽

...

Keyword(s):

Self Assembly ◽

Antitumor Effect ◽

Drug Loading ◽

Loading Efficiency ◽

Carrier Free ◽

Drug Loading Efficiency

Carrier-free paclitaxel nanoparticles with higher drug loading efficiency, less non-specific toxicity and more stable and durable antitumor effect of Ptx.

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Solvent Diffusion Method: An Effective Approach to Formulate Nanosponges Loaded with Naproxen Sodium

RADS Journal of Pharmacy and Pharmaceutical Sciences ◽

10.37962/jpps.v8i2.338 ◽

2020 ◽

Vol 8 (2) ◽

pp. 74-80

Author(s):

Fizza Ilyas ◽

Muhammad Jamsahid ◽

Irfan Bashir ◽

Rabia Aslam ◽

Tooba Mehboob ◽

...

Keyword(s):

Zeta Potential ◽

Naproxen Sodium ◽

Active Drug ◽

Drug Loading ◽

Study Drug ◽

Diffusion Method ◽

Diffusion Study ◽

Franz Cell ◽

Loading Efficiency ◽

Drug Loading Efficiency

Objective: Solubility of naproxen sodium is limited. In conventional dosage form it causes different gastro intestinal problems. To overcome these difficulties naproxen sodium loaded nano sponges were designed. Methodology: Nanosponges were formulated by using emulsion solvent evaporation technique. To obtain dispersion of nanosponges, homogenization of active drug, with specified quantities of polyvinyl alcohol, dichloromethane, ethyl cellulose and distilled, water was done. Compatibility among excipients and active drug was checked by FTIR and results didn’t show any interaction between them. 11 trial formulations were tested for poly dispersity, zeta potential, particle size and viscosity. Results: Results showed all formulations except NS9, NS10 and NS11 were in nano range. Formulation NS1 to NS6 fall in category of “mid poly dispersity” and formulation NS7 to NS11 were in the category of “very poly dispersity”. Values of Zeta potential of all formulations were in negative range -0.106 to -9.75 mV. The value of viscosity of all formulations were 0.8872. NS2 and NS3 were selected for further testing like Franz cell diffusion study, stability testing and drug loading efficiency. In Franz cell diffusion study, drug release for NS2= 89.62%, for NS3= 89.10% at 50 minutes’ time. Stability studies performed for the 21 days, NS2 and NS3 revealed slight change in percentage drug content at 4°C and 25°C, and major changes were observed at 45°C temperature. Drug loading efficiency was found in NS2= 97.659 % and for NS3= 98.901%. Conclusion: Nanosponges formulations loaded with naproxen sodium have successfully been prepared.

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