Preliminary pharmacokinetics of PEGylated oxaliplatin polylactic acid nanoparticles in rabbits and tumor-bearing mice

Wei, Haitian; Xu, Lisa X.; Sun, Yong; Li, Gaohong; Cui, Zhaoyuan; Yan, Guowen; Chen, Qian; Yin, Hongli; Ma, Chao

doi:10.3109/21691401.2014.883402

Cited by 8 publications

(4 citation statements)

References 10 publications

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“…The drug release method and its approach from the in vitro release study were confirmed by integrating it into kinetic models (0 order, 1 st order, Higuchi's, and Korsemeyer Peppa's model). The fitting curve technique understood CAP release through micelle formulation [38]. Results obtained through in vitro release studies were verified with different kinetic equations [39].…”

Section: Drug Release Kineticsmentioning

confidence: 87%

QBD Approach for the Development of Capsaicin-Loaded Glycyrrhetinic Acid Conjugated Stearic Acid Grafted Chitosan Polymeric Micelles for Active Hepatic Targeting

Konda

2023

Int J App Pharm

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Objective: Capsaicin (CAP) is a naturally occurring alkaloid forecasted in the treatment of Alcoholic Hepatitis (AH), but least studied due to its hydrophobicity, low bioavailability, and less target-specific release. Hence, the present study aimed to synthesize glycyrrhetinic acid conjugated stearic acid grafted chitosan (GA-CS-g-SA) and prepare CAP-loaded GA-CS-g-SA micelles. Methods: Quality by design (QbD) approach in coordination with "Box-Behnken Designs (BBD)" was used to optimize the process parameters. GA-CS-g-SA was synthesized and characterized for its physic-chemical. Results: The "Proton Nuclear Magnetic Resonance (1H NMR)" spectrum depicted a strong signal at d=1.0 ppm and endorsed to-CH2 group of SA and d=3.5-3.65 ppm depicting GA, which confirms the formation of GA-CS-g-SA. Critical micellar concentration (CMC) was found to be 13.45±1.72 µg/ml and amino groups substitute degree (SD %) was 10.12%±1.09%, indicating successful linkage of GA and SA on CS. The prominent peaks of CAP (0.9 and 1.31 ppm) in 1H NMR spectra disappeared, indicating drug loading in the micellar core. Micelle's normal particle range was 167.54 nm, and encapsulation efficiency was 67.85%. The CAP-GA-CS-g-SA was found to be biocompatible following the hemolysis test. In vitro release pattern showed 78.68±3.12% in 24h, indicating the slower release of CAP from micelle, whereas 99.48±2.56% was released from non-micellar formulations in 6 h. CAP release from drug-loaded micelles showed a biphasic model with an early burst release in four hours, following a slower and sustained release pattern till 24h. Conclusion: CAP-GA-CS-g-SA micelle is a hopeful advancement to progress bioavailability and controlled release of highly hydrophobic CAP. Further in vivo studies would be evident for targeting hepatocytes and treating AH using CAP-GA-CS-g-SA.

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Section: Drug Release Kineticsmentioning

confidence: 87%

QBD Approach for the Development of Capsaicin-Loaded Glycyrrhetinic Acid Conjugated Stearic Acid Grafted Chitosan Polymeric Micelles for Active Hepatic Targeting

Konda

2023

Int J App Pharm

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“…The fitting curve technique understood CAP release through micelle formulation [36]. Results obtained through in vitro release studies were verified with different kinetic equations.…”

Section: Drug Release Kineticsmentioning

confidence: 91%

QBD Approach for the Development of Capsaicin-Loaded Stearic Acid-Grafted Chitosan Polymeric Micelles

Konda

Sampathi

2023

Int J App Pharm

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Objective: Capsaicin (CAP) is a naturally occurring alkaloid forecasted in the treatment of Alcoholic Hepatitis (AH), but least studied due to its hydrophobicity and low bioavailability. Hence, the present study aimed to optimize the parameters for the synthesis of stearic acid grafted chitosan (CS-g-SA) copolymer and preparation of CAP-loaded CS-g-SA micelles. Methods: Quality by design (QbD) approach in coordination with “Central composite designs (CCD) and Box–Behnken designs (BBD)” was used to optimize the process parameters. Results: CS-g-SA was synthesized at 80 °C, 480 min, and 946 rpm, at these optimized conditions, the average particle size and practical yield were found to be 134.70 nm and 85.69%, respectively. Proton Nuclear Magnetic Resonance (1H NMR) spectra depicted a sharp signal at d=1.0 ppm endorsing to -CH2 group of SA and confirming the formation of CS-g-SA copolymer. Critical micellar concentration (CMC) and amino groups substitute degree (SD %) were found to be 30.3±1.51µg/ml and 21.3±0.58%, respectively. The distinguished peaks of CAP (0.9 and 1.31 ppm) in 1H NMR spectra disappeared, indicating drug loading in the micellar core. Micelles had an average particle size of 163.15 nm and an encapsulation efficiency of 68.45%. The CAP-CS-g-SA was found to be biocompatible in accordance with the hemolysis test. The in vitro release pattern showed 86.78 % in 24 h, indicating the slower release of CAP from micelle, whereas 99.48% CAP was released from non-micellar formulations in 6 h. Conclusion: CAP-CS-g-SA micelle is a promising approach to improve the bioavailability and controlled release of extremely hydrophobic CAP and further in vivo studies would be evident for the treatment of AH using CAP-CS-g-SA.

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“…The method was validated for selectivity, linearity, precision, accuracy, extract recovery, matrix effect and stability according to the FDA guideline for validation of bioanalytical methods [12,13]. Validation runs were conducted on three consecutive days.…”

Section: Methods Validationmentioning

confidence: 99%

Simultaneous determination of AM80 (tamibarotene) and WJD-A-1 in rat plasma by ultra high-performance liquid chromatography–tandem mass spectrometry and its application to a pharmacokinetic study

Leng

Zhao

et al. 2018

Artificial Cells, Nanomedicine, and Biotechnology

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A compound (WJD-A-1) was previously reported as a candidate prodrug of Am80 (tamibarotene), which was approved in Japan in 2005 as a therapeutic agent for recurrent refractory acute promyelocytic leukaemia. A rapid, selective and sensitive ultra high-performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS) method was developed for the first time to simultaneously determine WJD-A-1 and its major phase-I metabolites AM80 in rat plasma. After a simple sample preparation procedure by protein precipitation with methanol and acetonitrile, WJD-A-1, AM80 and the internal standard were chromatographed on an ACQUITY UPLC BEH C column. The mobile phase consisted of methanol-0.1% formic acid (80:20, v/v) and the flow rate was 0.20 mL/min. The detection was performed on a triple quadrupole tandem mass spectrometer by multiple reaction monitoring (MRM) mode via electrospray ionization (ESI) source. Each plasma sample was chromatographed within 2.6 min. The linear calibration curves for WJD-A-1 and the AM80 were obtained in the concentration range of 5.40-5.40 × 10 and 5.08-5.08 × 10 ng/mL, respectively (r ≥ 0.99). The intra- and inter-day precision (relative standard deviation, RSD) values were less than 8% and the accuracy (relative error, RE) was within ±6.8%, determined from quality control (QC) samples for the analytes. The method herein described was fully validated and successfully applied to pharmacokinetic study of WJD-A-1 following an intravenous administration of 300 μg/kg WJD-A-1 to rats.

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Preliminary pharmacokinetics of PEGylated oxaliplatin polylactic acid nanoparticles in rabbits and tumor-bearing mice

Cited by 8 publications

References 10 publications

QBD Approach for the Development of Capsaicin-Loaded Glycyrrhetinic Acid Conjugated Stearic Acid Grafted Chitosan Polymeric Micelles for Active Hepatic Targeting

QBD Approach for the Development of Capsaicin-Loaded Glycyrrhetinic Acid Conjugated Stearic Acid Grafted Chitosan Polymeric Micelles for Active Hepatic Targeting

QBD Approach for the Development of Capsaicin-Loaded Stearic Acid-Grafted Chitosan Polymeric Micelles

Simultaneous determination of AM80 (tamibarotene) and WJD-A-1 in rat plasma by ultra high-performance liquid chromatography–tandem mass spectrometry and its application to a pharmacokinetic study

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