Nanoparticles-based drug delivery systems have attracted significant attention in biomedical fields because they can deliver loaded cargoes to the target site in a controlled manner. However, tremendous challenges must still be overcome to reach the expected targeting and therapeutic efficacy
in vivo
. These challenges mainly arise because the interaction between nanoparticles and biological systems is complex and dynamic and is influenced by the physicochemical properties of the nanoparticles and the heterogeneity of biological systems. Importantly, once the nanoparticles are injected into the blood, a protein corona will inevitably form on the surface. The protein corona creates a new biological identity which plays a vital role in mediating the bio-nano interaction and determining the ultimate results. Thus, it is essential to understand how the protein corona affects the delivery journey of nanoparticles
in vivo
and what we can do to exploit the protein corona for better delivery efficiency. In this review, we first summarize the fundamental impact of the protein corona on the delivery journey of nanoparticles. Next, we emphasize the strategies that have been developed for tailoring and exploiting the protein corona to improve the transportation behavior of nanoparticles
in vivo
. Finally, we highlight what we need to do as a next step towards better understanding and exploitation of the protein corona. We hope these insights into the “Yin and Yang” effect of the protein corona will have profound implications for understanding the role of the protein corona in a wide range of nanoparticles.
This study was performed to explore factors influencing the release of the proton pump inhibitor omeprazole from entericcoated capsules in vitro and absorption in vivo in beagle dogs. Enteric-coated pellets with different enteric coating materials and coating levels were designed and prepared. All self-prepared formulations were characterized in vitro as well as in vivo and compared to the brand and generic commercial products. Evaluation of the corresponding release profiles suggested that coating material was the most critical factor. Enteric coating level determined the lag time before initiation of drug release, and subcoating level affected the drug release rate. Pharmacokinetic studies were performed in beagle dogs to further confirm the influence of formulation factors on drug absorption. Medium at pH 6.8 was a more biorelevant condition for in vitro drug release tests, although medium at pH 6.0 was better for discriminating release profiles of different formulations. A multiple level C in vitro/in vivo correlation was preliminarily established by which T max and C max of omeprazole formulations could be predicted with release parameters such as T lag and T 25 . These results may facilitate quality evaluation and potentially improve the clinical efficacy of generic omeprazole products.
Intelligent drug delivery system based on “stimulus-response” mode emerging a promising perspective in next generation lipid-based nanoparticle. Here, we classify signal sources into physical and physiological stimulation according to their origin. The physical signals include temperature, ultrasound, and electromagnetic wave, while physiological signals involve pH, redox condition, and associated proteins. We first summarize external physical response from three main points about efficiency, particle state, and on-demand release. Afterwards, we describe how to design drug delivery using the physiological environment in vivo and present different current application methods. Lastly, we draw a vision of possible future development.
We have previously established a type of anti-resistant stealth liposomal topotecan plus amlodipine for overcoming the multi-drug resistance (MDR) in resistant leukemia cells. The objective of the present study was to further characterize it in the diversified non-resistant solid tumors in vitro and in vivo. Stealth liposomal topotecan plus amlodipine was re-prepared and physicochemically characterized. The in vitro drug release assays of topotecan and amlodipine from liposomes were performed using a dialysis method. 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assays were performed in murine sarcoma S180 cells and human breast cancer MCF-7 cells, respectively. Apoptotic percentages of S180 cells were evaluated using flow cytometry. In vivo anti-tumor activity study and terminal deoxynucleotidyl transferase-mediated dUTP-biotin nick end labeling (TUNEL) analysis were performed in male Institute of Cancer Research (ICR) mice with S180 xenografts. Stealth liposomal topotecan plus amlodipine exhibited high drug encapsulation efficiencies, suitable particle size distribution, negatively charged zeta potential and prolonged release profiles for both topotecan and amlodipine. Amlodipine potentiated the antiproliferative effect and inducing apoptotic effect of topotecan on the tumor cells, exhibiting an additive anti-tumor effect. Stealth liposomal topotecan plus amlodipine showed the optimal anti-tumor activity and inducing apoptotic effect in the in vivo studies. Stealth liposomal topotecan plus amlodipine demonstrated an overt anti-tumor activity in non-resistant solid tumors, suggesting that it deserves further clinical evaluations.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.