Journal of Pharmaceutics & Drug Delivery Research is a subscription as well as open access journal which promotes rigorous research that makes a significant contribution in advancing knowledge for Drug Delivery Research.

Pharmaceutics is the discipline of pharmacy that deals with the process of turning a new chemical entity (NCE) or old drugs into a medication to be used safely and effectively by patients. It is also called the science of dosage form design. There are many chemicals with pharmacological properties, but need special measures to help them achieve therapeutically relevant amounts at their sites of action.

Nanoparticle Formulation of Brusatol: A Novel Therapeutic Option for Cancers

Challenges to the use of brusatol for cancer chemotherapy include its reversible and short-lived effect on Nrf2 which is limited to a few hours, its non-selective inhibition of protein synthesis which renders it potentially toxic to non-cancerous cells resulting in adverse effects and poor water solubility. A nanoparticle formulation of brusatol is expected to overcome these challenges and facilitate the clinical use of brusatol. In this proof-of-principle study, a brusatol-loaded nanoparticle formulation is developed and characterized.

Method: Brusatol-loaded mPEG-PLGA nanoparticles were prepared using the oil-in-water emulsification solvent diffusion method and characterized. The drug content of the nanoparticle formulation was determined by High Performance Liquid Chromatography. Toxicity of the brusatol-loaded nanoparticles in prostate cancer cell lines was evaluated over 120 hours using the Cell Titer 96® Non- Radioactive Cell Proliferation Assay and nanoparticle uptake was studied by confocal microscopy.

Results: Scanning electron microscopy revealed the formation of nanoparticles. The average hydrodynamic particle size is 309.23 ± 2.3 nm. The in vitro release isotherm showed a biphasic and sustained release of the encapsulated drug. Data from cytotoxicity studies reveal that the nanoparticle formulation showed more toxicity compared to control brusatol solution in PC-3 and LNCaP cell lines. Confocal microscopy studies showed internalization of the nanoparticles in PC-3 cells at 6 hours. In addition, z-stack images confirm the presence of nanoparticles at various depths within the cells

Conclusion: The stealth nanoparticle formulation allows the sustained release of brusatol with the potential to modulate its short-lived effect on Nrf2. In addition, the potential of the nanoparticle formulation to target the tumor microenvironment via the enhanced permeability and retention effect and prevent toxicity to noncancerous cells is achieved. We report the preparation and characterization of a stealth nanoparticle formulation of brusatol to facilitate the clinical use of the drug for the treatment of cancers.

Journal of Pharmaceutics & Drug Delivery Research (JPDDR) will consider manuscripts involving the Pharmaceutical Sciences, Biopharmaceutics, Aerosol Medicine, Microspheres, Controlled Release, Transdermal Patches, Natural Products, Drug Metabolism and all fields pertaining to the drug delivery & research. It accepts research, review papers, online letters to the editors & brief comments on previously published articles or other relevant findings in SciTechnol.

On the eve completing more than a decade in medical publishing the Journal of Pharmaceutics and Drug Delivery Research waives off 50% of its article processing charges to promote quality research from across the nations of the globe to encourage the latest research in the field of Pharmaceutics and Drugs only during manuscripts received on or before 28 December 2019 you may submit your manuscript either Online or via email mentioned below.

With Kind Regards,

Subhana Quadri

Journal Coordinator

Journal of Pharmaceutics & Drug Delivery Research

Email: pharmaceutics@scitecjournals.com

Journal of Pharmaceutics & Drug Delivery Research is a subscription as well as open access journal which promotes rigorous research that makes a significant contribution in advancing knowledge for Drug Delivery Research.

Pharmaceutics is the discipline of pharmacy that deals with the process of turning a new chemical entity (NCE) or old drugs into a medication to be used safely and effectively by patients. It is also called the science of dosage form design. There are many chemicals with pharmacological properties, but need special measures to help them achieve therapeutically relevant amounts at their sites of action.

Nanoparticle Formulation of Brusatol: A Novel Therapeutic Option for Cancers

Challenges to the use of brusatol for cancer chemotherapy include its reversible and short-lived effect on Nrf2 which is limited to a few hours, its non-selective inhibition of protein synthesis which renders it potentially toxic to non-cancerous cells resulting in adverse effects and poor water solubility. A nanoparticle formulation of brusatol is expected to overcome these challenges and facilitate the clinical use of brusatol. In this proof-of-principle study, a brusatol-loaded nanoparticle formulation is developed and characterized.

Method: Brusatol-loaded mPEG-PLGA nanoparticles were prepared using the oil-in-water emulsification solvent diffusion method and characterized. The drug content of the nanoparticle formulation was determined by High Performance Liquid Chromatography. Toxicity of the brusatol-loaded nanoparticles in prostate cancer cell lines was evaluated over 120 hours using the Cell Titer 96® Non- Radioactive Cell Proliferation Assay and nanoparticle uptake was studied by confocal microscopy.

Results: Scanning electron microscopy revealed the formation of nanoparticles. The average hydrodynamic particle size is 309.23 ± 2.3 nm. The in vitro release isotherm showed a biphasic and sustained release of the encapsulated drug. Data from cytotoxicity studies reveal that the nanoparticle formulation showed more toxicity compared to control brusatol solution in PC-3 and LNCaP cell lines. Confocal microscopy studies showed internalization of the nanoparticles in PC-3 cells at 6 hours. In addition, z-stack images confirm the presence of nanoparticles at various depths within the cells

Conclusion: The stealth nanoparticle formulation allows the sustained release of brusatol with the potential to modulate its short-lived effect on Nrf2. In addition, the potential of the nanoparticle formulation to target the tumor microenvironment via the enhanced permeability and retention effect and prevent toxicity to noncancerous cells is achieved. We report the preparation and characterization of a stealth nanoparticle formulation of brusatol to facilitate the clinical use of the drug for the treatment of cancers.

Journal of Pharmaceutics & Drug Delivery Research (JPDDR) will consider manuscripts involving the Pharmaceutical Sciences, Biopharmaceutics, Aerosol Medicine, Microspheres, Controlled Release, Transdermal Patches, Natural Products, Drug Metabolism and all fields pertaining to the drug delivery & research. It accepts research, review papers, online letters to the editors & brief comments on previously published articles or other relevant findings in SciTechnol.

On the eve completing more than a decade in medical publishing the Journal of Pharmaceutics and Drug Delivery Research waives off 50% of its article processing charges to promote quality research from across the nations of the globe to encourage the latest research in the field of Pharmaceutics and Drugs only during manuscripts received on or before 28 December 2019 you may submit your manuscript either Online or via email mentioned below.

With Kind Regards,

Subhana Quadri

Journal Coordinator

Journal of Pharmaceutics & Drug Delivery Research

Email: pharmaceutics@scitecjournals.com