BRAIN TARGETING OF 1,9-PYRAZOLOANTHRONE AN C-JUN-N-TERMINAL KINASE INHIBITOR USING LIPOSOMES FOR EFFECTIVE MANAGEMENT OF PARKINSON’S DISEASE

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SUDHAKAR AMBHORE NILESH; SATYANARAYANA RAJU KALIDHINDI RAMA; MULUKUTLA SHASHANK; YAMJALA KARTHIK; MOHIRE SHUBHASHRI; SATYANARAYANA REDDY KARRI VEERA VENKATA; GUPTA SAURABH; MURTHY VISHAKANTHA; ELANGO KANNAN

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Journal: Iranian Journal of Pharmaceutical Research Year:2017 | Volume:16 | Issue:4 Page(s): 1463-1478

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Title

BRAIN TARGETING OF 1,9-PYRAZOLOANTHRONE AN C-JUN-N-TERMINAL KINASE INHIBITOR USING LIPOSOMES FOR EFFECTIVE MANAGEMENT OF PARKINSON’S DISEASE

Author(s)

Keywords

PARKINSON'S DISEASE

9-PYRAZOLOANTHRONE

BRAIN TARGETING

BIODISTRIBUTION

LIPOSOMES

SUSTAINED- RELEASE SYSTEM

SH-SY5Y NEUROBLASTOMA CELL LINE

Abstract

The major challenge to treat Parkinson’s disease (PD) is penetration of target molecule into the brain to improve the efficacy of drugs. To achieve better brain penetration and targeted delivery, 1, 9-PYRAZOLOANTHRONE (1, 9-P) loaded LIPOSOMES were developed by solvent injection technique using ultrasonication and evaluated for particle size, morphology, entrapment efficiency, FT-IR, and in-vitro drug release studies. The potential of 1, 9-PYRAZOLOANTHRONE (1, 9- P), a c-Jun-N-terminal Kinase (JNK-3) inhibitor which could stop or retard the rate of apoptosis of neuronal cells was also evaluated. In-vivo pharmacokinetic and brain uptake studies of LIPOSOMES were performed to investigate the bioavailability and brain distribution of 1, 9-P. Cytotoxicity and neuroprotection were done on SH-SY5Y cell line using MTT and AO/EB apoptosis assay. The optimized batch of LIPOSOMES showed an average size of 112.33±0.84 nm with a zeta potential value of -19.40 mV and 78.96±0.28% drug entrapment efficiency. The in-vitro release studies demonstrated the sustained release profile of liposome up to 24 h. The pharmacokinetic data in Wistar rats over the period of 12 h demonstrated 4.82-folds greater AUC(0-12 h) for liposome in brain compared with 1, 9-P suspension. Cytotoxicity assay showed no sign of toxicity, whereas apoptosis assay revealed a neuroprotective action of LIPOSOMES. The results demonstrated successful targeting of the 1, 9-P, to brain as a novel strategy having significant therapeutic potential to treat PD.

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APA: Copy

SUDHAKAR AMBHORE, NILESH, SATYANARAYANA RAJU, KALIDHINDI RAMA, MULUKUTLA, SHASHANK, YAMJALA, KARTHIK, MOHIRE, SHUBHASHRI, SATYANARAYANA REDDY KARRI, VEERA VENKATA, GUPTA, SAURABH, MURTHY, VISHAKANTHA, & ELANGO, KANNAN. (2017). BRAIN TARGETING OF 1,9-PYRAZOLOANTHRONE AN C-JUN-N-TERMINAL KINASE INHIBITOR USING LIPOSOMES FOR EFFECTIVE MANAGEMENT OF PARKINSON’S DISEASE. IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH (IJPR), 16(4), 1463-1478. SID. https://sid.ir/paper/288744/en

Vancouver: Copy

SUDHAKAR AMBHORE NILESH, SATYANARAYANA RAJU KALIDHINDI RAMA, MULUKUTLA SHASHANK, YAMJALA KARTHIK, MOHIRE SHUBHASHRI, SATYANARAYANA REDDY KARRI VEERA VENKATA, GUPTA SAURABH, MURTHY VISHAKANTHA, ELANGO KANNAN. BRAIN TARGETING OF 1,9-PYRAZOLOANTHRONE AN C-JUN-N-TERMINAL KINASE INHIBITOR USING LIPOSOMES FOR EFFECTIVE MANAGEMENT OF PARKINSON’S DISEASE. IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH (IJPR)[Internet]. 2017;16(4):1463-1478. Available from: https://sid.ir/paper/288744/en

IEEE: Copy

NILESH SUDHAKAR AMBHORE, KALIDHINDI RAMA SATYANARAYANA RAJU, SHASHANK MULUKUTLA, KARTHIK YAMJALA, SHUBHASHRI MOHIRE, VEERA VENKATA SATYANARAYANA REDDY KARRI, SAURABH GUPTA, VISHAKANTHA MURTHY, and KANNAN ELANGO, “BRAIN TARGETING OF 1,9-PYRAZOLOANTHRONE AN C-JUN-N-TERMINAL KINASE INHIBITOR USING LIPOSOMES FOR EFFECTIVE MANAGEMENT OF PARKINSON’S DISEASE,” IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH (IJPR), vol. 16, no. 4, pp. 1463–1478, 2017, [Online]. Available: https://sid.ir/paper/288744/en

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