Augumented bioavailability of maltodextrin-based Tenofovir proniosomes via inhibition of MDR1 mediated transport efflux

Anka Rao Aretı

Makale detayları

Augumented bioavailability of maltodextrin-based Tenofovir proniosomes via inhibition of MDR1 mediated transport efflux

Yazarlar:

Anka Rao Aretı

Yayıncı:

Marmara University

Ana Başlıklar:

Pharmaceutical Sciences | Pharmaceutical Delivery Technologies

Dergi:

Journal of Research in Pharmacy Vol.28 Issue 5, pp.1357-1368

Belge Tipi:

Makale

Yayın Tarihi:

6/2025

Belge Dili:

İngilizce

Document ID (Org No.):

2001347567

pISSN:

2630-6344

Anahtar kelimeler:

Özet:

 Tenofovir is an antiviral drug indicated for the treatment of infections caused by the human immunodeficiency virus HIV and hepatitis B virus HBV. TNF is classified as a BCS Class III drug, indicating its ability to readily dissolve in gastrointestinal fluids with poor permeability across intestinal membranes results in a lower absorption rate, ultimately restricting its bioavailability. The primary challenges associated to enhancing the bioavailability of TNF involve intestinal degradation and efflux transport facilitated by Multidrug resistance protein1. TNF-loaded proniosomes were formulated using 32 factorial design by applying slurry method of preparation with a molar ratio of 2.5:1:1.5 for cholesterol, span 60, and maltodextrin, respectively. Maltodextrin-based polymeric nanoparticles exhibited desirable nano-scale properties, including size, polydispersity index, and zeta potentials, which fell within acceptable ranges. The successful PNFs T-PN3, T-PN4, and T-PN7 demonstrated TNF entrapment in the range of 92.96 to 96.28. The hydration volume and hydration time of proniosome-based niosomes for delivering TNF were optimized and the results demonstrated the structural homogeneity of niosomes derived from proniosomes. Transmission electron microscopy TEM analysis indicated that the niosomes exhibit a uniform and smooth surface morphology. Successful formulations were further characterized for their powder behaviour by angle of repose, TNF interactions with formulation components by FT-IR and DSC thermal analysis. The T-PN3 and T-PN7 formulations demonstrated a high in-vitro release rate of approximately 99 in PBS. Additionally, the cellular uptake of TNF from successful PNFs in NCI-N87 cells ranged from 81 to 83, indicating that T-PN3 and T-PN7 exhibited superior performance compared to free TNF and the commercially available tenofovir. Further mechanistic analysis was conducted using MDR1 efflux studies and western blot techniques. The results demonstrated that both T-PN3 and T-PN7 effectively inhibited the efflux transport of TNF through MDR1 in MDCK-MDR1 and Caco-2 cells.

 Tenofovir is an antiviral drug indicated for the treatment of infections caused by the human immunodeficiency virus HIV and hepatitis B virus HBV. TNF is classified as a BCS Class III drug, indicating its ability to readily dissolve in gastrointestinal fluids with poor permeability across intestinal membranes results in a lower absorption rate, ultimately restricting its bioavailability. The primary challenges associated to enhancing the bioavailability of TNF involve intestinal degradation and efflux transport facilitated by Multidrug resistance protein1. TNF-loaded proniosomes were formulated using 32 factorial design by applying slurry method of preparation with a molar ratio of 2.5:1:1.5 for cholesterol, span 60, and maltodextrin, respectively. Maltodextrin-based polymeric nanoparticles exhibited desirable nano-scale properties, including size, polydispersity index, and zeta potentials, which fell within acceptable ranges. The successful PNFs T-PN3, T-PN4, and T-PN7 demonstrated TNF entrapment in the range of 92.96 to 96.28. The hydration volume and hydration time of proniosome-based niosomes for delivering TNF were optimized and the results demonstrated the structural homogeneity of niosomes derived from proniosomes. Transmission electron microscopy TEM analysis indicated that the niosomes exhibit a uniform and smooth surface morphology. Successful formulations were further characterized for their powder behaviour by angle of repose, TNF interactions with formulation components by FT-IR and DSC thermal analysis. The T-PN3 and T-PN7 formulations demonstrated a high in-vitro release rate of approximately 99 in PBS. Additionally, the cellular uptake of TNF from successful PNFs in NCI-N87 cells ranged from 81 to 83, indicating that T-PN3 and T-PN7 exhibited superior performance compared to free TNF and the commercially available tenofovir. Further mechanistic analysis was conducted using MDR1 efflux studies and western blot techniques. The results demonstrated that both T-PN3 and T-PN7 effectively inhibited the efflux transport of TNF through MDR1 in MDCK-MDR1 and Caco-2 cells.

 Tenofovir is an antiviral drug indicated for the treatment of infections caused by the human immunodeficiency virus HIV and hepatitis B virus HBV. TNF is classified as a BCS Class III drug, indicating its ability to readily dissolve in gastrointestinal fluids with poor permeability across intestinal membranes results in a lower absorption rate, ultimately restricting its bioavailability. The primary challenges associated to enhancing the bioavailability of TNF involve intestinal degradation and efflux transport facilitated by Multidrug resistance protein1. TNF-loaded proniosomes were formulated using 32 factorial design by applying slurry method of preparation with a molar ratio of 2.5:1:1.5 for cholesterol, span 60, and maltodextrin, respectively. Maltodextrin-based polymeric nanoparticles exhibited desirable nano-scale properties, including size, polydispersity index, and zeta potentials, which fell within acceptable ranges. The successful PNFs T-PN3, T-PN4, and T-PN7 demonstrated TNF entrapment in the range of 92.96 to 96.28. The hydration volume and hydration time of proniosome-based niosomes for delivering TNF were optimized and the results demonstrated the structural homogeneity of niosomes derived from proniosomes. Transmission electron microscopy TEM analysis indicated that the niosomes exhibit a uniform and smooth surface morphology. Successful formulations were further characterized for their powder behaviour by angle of repose, TNF interactions with formulation components by FT-IR and DSC thermal analysis. The T-PN3 and T-PN7 formulations demonstrated a high in-vitro release rate of approximately 99 in PBS. Additionally, the cellular uptake of TNF from successful PNFs in NCI-N87 cells ranged from 81 to 83, indicating that T-PN3 and T-PN7 exhibited superior performance compared to free TNF and the commercially available tenofovir. Further mechanistic analysis was conducted using MDR1 efflux studies and western blot techniques. The results demonstrated that both T-PN3 and T-PN7 effectively inhibited the efflux transport of TNF through MDR1 in MDCK-MDR1 and Caco-2 cells.

 Tenofovir is an antiviral drug indicated for the treatment of infections caused by the human immunodeficiency virus HIV and hepatitis B virus HBV. TNF is classified as a BCS Class III drug, indicating its ability to readily dissolve in gastrointestinal fluids with poor permeability across intestinal membranes results in a lower absorption rate, ultimately restricting its bioavailability. The primary challenges associated to enhancing the bioavailability of TNF involve intestinal degradation and efflux transport facilitated by Multidrug resistance protein1. TNF-loaded proniosomes were formulated using 32 factorial design by applying slurry method of preparation with a molar ratio of 2.5:1:1.5 for cholesterol, span 60, and maltodextrin, respectively. Maltodextrin-based polymeric nanoparticles exhibited desirable nano-scale properties, including size, polydispersity index, and zeta potentials, which fell within acceptable ranges. The successful PNFs T-PN3, T-PN4, and T-PN7 demonstrated TNF entrapment in the range of 92.96 to 96.28. The hydration volume and hydration time of proniosome-based niosomes for delivering TNF were optimized and the results demonstrated the structural homogeneity of niosomes derived from proniosomes. Transmission electron microscopy TEM analysis indicated that the niosomes exhibit a uniform and smooth surface morphology. Successful formulations were further characterized for their powder behaviour by angle of repose, TNF interactions with formulation components by FT-IR and DSC thermal analysis. The T-PN3 and T-PN7 formulations demonstrated a high in-vitro release rate of approximately 99 in PBS. Additionally, the cellular uptake of TNF from successful PNFs in NCI-N87 cells ranged from 81 to 83, indicating that T-PN3 and T-PN7 exhibited superior performance compared to free TNF and the commercially available tenofovir. Further mechanistic analysis was conducted using MDR1 efflux studies and western blot techniques. The results demonstrated that both T-PN3 and T-PN7 effectively inhibited the efflux transport of TNF through MDR1 in MDCK-MDR1 and Caco-2 cells.

Makale detayları

Augumented bioavailability of maltodextrin-based Tenofovir proniosomes via inhibition of MDR1 mediated transport efflux

Yazarlar:

Anka Rao Aretı

Yayıncı:

Marmara University

Ana Başlıklar:

Pharmaceutical Sciences | Pharmaceutical Delivery Technologies

Dergi:

Journal of Research in Pharmacy Vol.28 Issue 5, pp.1357-1368

Belge Tipi:

Makale

Yayın Tarihi:

6/2025

Belge Dili:

İngilizce

Document ID (Org No.):

2001347567

pISSN:

2630-6344

Tenofovir

Proniosomes

Niosomes

MDR-mediated drug efflux

Slurry technique

Sayı

Makale detayları

Augumented bioavailability of maltodextrin-based Tenofovir proniosomes via inhibition of MDR1 mediated transport efflux

Yazarlar: Anka Rao Aretı

Yayıncı: Marmara University

Ana Başlıklar: Pharmaceutical Sciences | Pharmaceutical Delivery Technologies

Dergi: Journal of Research in Pharmacy Vol.28 Issue 5, pp.1357-1368

Belge Tipi: Makale

Yayın Tarihi: 6/2025

Belge Dili: İngilizce

Document ID (Org No.): 2001347567

pISSN: 2630-6344

Tenofovir

Proniosomes

Niosomes

MDR-mediated drug efflux

Slurry technique

Sayı

Yazarlar:

Anka Rao Aretı

Yayıncı:

Marmara University

Ana Başlıklar:

Pharmaceutical Sciences | Pharmaceutical Delivery Technologies

Dergi:

Journal of Research in Pharmacy Vol.28 Issue 5, pp.1357-1368

Belge Tipi:

Makale

Yayın Tarihi:

6/2025

Belge Dili:

İngilizce

Document ID (Org No.):

2001347567

pISSN:

2630-6344