Tags

Type your tag names separated by a space and hit enter

Surface engineered nanoliposomal platform for selective lymphatic uptake of asenapine maleate: In vitro and in vivo studies.
Mater Sci Eng C Mater Biol Appl. 2020 Apr; 109:110620.MS

Abstract

Asenapine maleate (ASPM) is an antipsychotic drug prescribed for the treatment of schizophrenia and bipolar disorder. ASPM possesses low oral bioavailability due to extensive hepatic metabolism. Therefore, RGD peptide conjugated liposomes loaded with ASPM were prepared to target Peyer's patches in the intestine which in-turn get access into intestinal lymphatic system thereby increasing the oral bioavailability of the drug. Liposomes were evaluated for size, zeta potential, differential scanning calorimetry (DSC), FTIR spectroscopy, X-ray diffraction (XRD), shape and morphology, in vitro drug release, cell line studies, everted intestinal uptake, pharmacodynamics, pharmacokinetics, tissue distribution, targetability and stability studies. In vitro drug release study showed the sustained release of drug from the formulations. Optimized liposomes (size <110 nm) showed greater permeability across the Caco2 + Raji B co-culture model in vitro and everted rat ileum ex vivo. Liposomes showed increase in bioavailability and high efficacy in reducing the L-DOPA-carbidopa induced locomotor count compared to plain drug. Liposomes also showed high concentration of drug in the brain after their oral administration. Imaging studies showed that RGD peptide conjugated liposomes were successful in targeting the Peyer's patches, both in vivo and ex vivo. The study successfully demonstrated the improved pharmacokinetics and efficacy profile of ASPM by using a ligand conjugated targeted liposomal system.

Authors+Show Affiliations

Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal 576104, Karnataka State, India.School of Cancer and Pharmaceutical Sciences, King's College London, Franklin-Wilkins Building, 150 Stamford Street, London SE1 9NH, UK.School of Cancer and Pharmaceutical Sciences, King's College London, Franklin-Wilkins Building, 150 Stamford Street, London SE1 9NH, UK.Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal 576104, Karnataka State, India.Centre for Pharmaceutical Nanotechnology, Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research, Sector 67, S.A.S. Nagar, Mohali, Punjab 160062, India.School of Cancer and Pharmaceutical Sciences, King's College London, Franklin-Wilkins Building, 150 Stamford Street, London SE1 9NH, UK.Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal 576104, Karnataka State, India. Electronic address: ss.mutalik@manipal.edu.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

32228915

Citation

Managuli, Renuka S., et al. "Surface Engineered Nanoliposomal Platform for Selective Lymphatic Uptake of Asenapine Maleate: in Vitro and in Vivo Studies." Materials Science & Engineering. C, Materials for Biological Applications, vol. 109, 2020, p. 110620.
Managuli RS, Wang JT, Faruqu FM, et al. Surface engineered nanoliposomal platform for selective lymphatic uptake of asenapine maleate: In vitro and in vivo studies. Mater Sci Eng C Mater Biol Appl. 2020;109:110620.
Managuli, R. S., Wang, J. T., Faruqu, F. M., Pandey, A., Jain, S., Al-Jamal, K. T., & Mutalik, S. (2020). Surface engineered nanoliposomal platform for selective lymphatic uptake of asenapine maleate: In vitro and in vivo studies. Materials Science & Engineering. C, Materials for Biological Applications, 109, 110620. https://doi.org/10.1016/j.msec.2019.110620
Managuli RS, et al. Surface Engineered Nanoliposomal Platform for Selective Lymphatic Uptake of Asenapine Maleate: in Vitro and in Vivo Studies. Mater Sci Eng C Mater Biol Appl. 2020;109:110620. PubMed PMID: 32228915.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Surface engineered nanoliposomal platform for selective lymphatic uptake of asenapine maleate: In vitro and in vivo studies. AU - Managuli,Renuka S, AU - Wang,Julie Tzu-Wen, AU - Faruqu,Farid Muhammad, AU - Pandey,Abhjieet, AU - Jain,Sanyog, AU - Al-Jamal,Khuloud T, AU - Mutalik,Srinivas, Y1 - 2020/01/07/ PY - 2019/08/02/received PY - 2019/12/31/revised PY - 2019/12/31/accepted PY - 2020/4/2/entrez KW - Asenapine maleate KW - Liposomes KW - Peyer's patches KW - RGD peptide SP - 110620 EP - 110620 JF - Materials science & engineering. C, Materials for biological applications JO - Mater Sci Eng C Mater Biol Appl VL - 109 N2 - Asenapine maleate (ASPM) is an antipsychotic drug prescribed for the treatment of schizophrenia and bipolar disorder. ASPM possesses low oral bioavailability due to extensive hepatic metabolism. Therefore, RGD peptide conjugated liposomes loaded with ASPM were prepared to target Peyer's patches in the intestine which in-turn get access into intestinal lymphatic system thereby increasing the oral bioavailability of the drug. Liposomes were evaluated for size, zeta potential, differential scanning calorimetry (DSC), FTIR spectroscopy, X-ray diffraction (XRD), shape and morphology, in vitro drug release, cell line studies, everted intestinal uptake, pharmacodynamics, pharmacokinetics, tissue distribution, targetability and stability studies. In vitro drug release study showed the sustained release of drug from the formulations. Optimized liposomes (size <110 nm) showed greater permeability across the Caco2 + Raji B co-culture model in vitro and everted rat ileum ex vivo. Liposomes showed increase in bioavailability and high efficacy in reducing the L-DOPA-carbidopa induced locomotor count compared to plain drug. Liposomes also showed high concentration of drug in the brain after their oral administration. Imaging studies showed that RGD peptide conjugated liposomes were successful in targeting the Peyer's patches, both in vivo and ex vivo. The study successfully demonstrated the improved pharmacokinetics and efficacy profile of ASPM by using a ligand conjugated targeted liposomal system. SN - 1873-0191 UR - https://www.unboundmedicine.com/medline/citation/32228915/Surface_engineered_nanoliposomal_platform_for_selective_lymphatic_uptake_of_asenapine_maleate:_In_vitro_and_in_vivo_studies L2 - https://linkinghub.elsevier.com/retrieve/pii/S0928-4931(19)32834-6 DB - PRIME DP - Unbound Medicine ER -
Try the Free App:
Prime PubMed app for iOS iPhone iPad
Prime PubMed app for Android
Prime PubMed is provided
free to individuals by:
Unbound Medicine.