Formulation and evaluation of lipid–polymeric hybrid nanovesicles for valsartan delivery: Bridging in vitro and in vivo Pharmacokinetics

Sayani Bhattacharyya; Maithili Sinha; Sweta Jha

Makale detayları

Formulation and evaluation of lipid–polymeric hybrid nanovesicles for valsartan delivery: Bridging in vitro and in vivo Pharmacokinetics

Yazarlar:

Sayani Bhattacharyya | Maithili Sinha | Sweta Jha

Yayıncı:

Hacettepe University

Ana Başlıklar:

Pharmaceutical Sciences | Pharmaceutical Delivery Technologies

Dergi:

Hacettepe University Journal of the Faculty of Pharmacy Vol.45 Issue 3, pp.211-222

Belge Tipi:

Makale

Yayın Tarihi:

1/2025

Belge Dili:

İngilizce

Document ID (Org No.):

2001357020

pISSN:

2458-8806

Anahtar kelimeler:

Özet:

 Hypertension, a leading global health concern, is associated with severe cardiovascular complications. Valsartan VAS, an angiotensin II receptor blocker, is a preferred antihypertensive medication with limited oral bioavailability 23 due to first-pass metabolism and P-glycoprotein p-gp efflux. This study developed lipid-polymeric hybrid nanovesicles of VAS using Eudragit RL100 and PEG 4000 to overcome these barriers. Lipid-polymeric nanovesicles P1-P3 were prepared by thin-film hydration combined with solvent evaporation techniques and evaluated for drug entrapment, particle size, zeta potential, and release kinetics. Formulation P3 at Eudragit RL100:PEG 4000 in a 2:1 ratio demonstrated superior entrapment efficiency 76, nanoscale size 140 nm, and stability, achieving a 6-fold increase in AUC compared to pure VAS. In vitro and ex vivo studies showed sustained release and enhanced intestinal permeation, with P3 achieving a 3.25-fold higher permeability. Pharmacokinetic studies confirmed enhanced bioavailability, reduced clearance, and prolonged retention. These findings underscore lipid-polymeric nanovesicles as a promising delivery system for poorly soluble drugs like VAS, addressing bioavailability challenges effectively.

 Hypertension, a leading global health concern, is associated with severe cardiovascular complications. Valsartan VAS, an angiotensin II receptor blocker, is a preferred antihypertensive medication with limited oral bioavailability 23 due to first-pass metabolism and P-glycoprotein p-gp efflux. This study developed lipid-polymeric hybrid nanovesicles of VAS using Eudragit RL100 and PEG 4000 to overcome these barriers. Lipid-polymeric nanovesicles P1-P3 were prepared by thin-film hydration combined with solvent evaporation techniques and evaluated for drug entrapment, particle size, zeta potential, and release kinetics. Formulation P3 at Eudragit RL100:PEG 4000 in a 2:1 ratio demonstrated superior entrapment efficiency 76, nanoscale size 140 nm, and stability, achieving a 6-fold increase in AUC compared to pure VAS. In vitro and ex vivo studies showed sustained release and enhanced intestinal permeation, with P3 achieving a 3.25-fold higher permeability. Pharmacokinetic studies confirmed enhanced bioavailability, reduced clearance, and prolonged retention. These findings underscore lipid-polymeric nanovesicles as a promising delivery system for poorly soluble drugs like VAS, addressing bioavailability challenges effectively.

 Hypertension, a leading global health concern, is associated with severe cardiovascular complications. Valsartan VAS, an angiotensin II receptor blocker, is a preferred antihypertensive medication with limited oral bioavailability 23 due to first-pass metabolism and P-glycoprotein p-gp efflux. This study developed lipid-polymeric hybrid nanovesicles of VAS using Eudragit RL100 and PEG 4000 to overcome these barriers. Lipid-polymeric nanovesicles P1-P3 were prepared by thin-film hydration combined with solvent evaporation techniques and evaluated for drug entrapment, particle size, zeta potential, and release kinetics. Formulation P3 at Eudragit RL100:PEG 4000 in a 2:1 ratio demonstrated superior entrapment efficiency 76, nanoscale size 140 nm, and stability, achieving a 6-fold increase in AUC compared to pure VAS. In vitro and ex vivo studies showed sustained release and enhanced intestinal permeation, with P3 achieving a 3.25-fold higher permeability. Pharmacokinetic studies confirmed enhanced bioavailability, reduced clearance, and prolonged retention. These findings underscore lipid-polymeric nanovesicles as a promising delivery system for poorly soluble drugs like VAS, addressing bioavailability challenges effectively.

 Hypertension, a leading global health concern, is associated with severe cardiovascular complications. Valsartan VAS, an angiotensin II receptor blocker, is a preferred antihypertensive medication with limited oral bioavailability 23 due to first-pass metabolism and P-glycoprotein p-gp efflux. This study developed lipid-polymeric hybrid nanovesicles of VAS using Eudragit RL100 and PEG 4000 to overcome these barriers. Lipid-polymeric nanovesicles P1-P3 were prepared by thin-film hydration combined with solvent evaporation techniques and evaluated for drug entrapment, particle size, zeta potential, and release kinetics. Formulation P3 at Eudragit RL100:PEG 4000 in a 2:1 ratio demonstrated superior entrapment efficiency 76, nanoscale size 140 nm, and stability, achieving a 6-fold increase in AUC compared to pure VAS. In vitro and ex vivo studies showed sustained release and enhanced intestinal permeation, with P3 achieving a 3.25-fold higher permeability. Pharmacokinetic studies confirmed enhanced bioavailability, reduced clearance, and prolonged retention. These findings underscore lipid-polymeric nanovesicles as a promising delivery system for poorly soluble drugs like VAS, addressing bioavailability challenges effectively.

Makale detayları

Formulation and evaluation of lipid–polymeric hybrid nanovesicles for valsartan delivery: Bridging in vitro and in vivo Pharmacokinetics

Yazarlar:

Sayani Bhattacharyya | Maithili Sinha | Sweta Jha

Yayıncı:

Hacettepe University

Ana Başlıklar:

Pharmaceutical Sciences | Pharmaceutical Delivery Technologies

Dergi:

Hacettepe University Journal of the Faculty of Pharmacy Vol.45 Issue 3, pp.211-222

Belge Tipi:

Makale

Yayın Tarihi:

1/2025

Belge Dili:

İngilizce

Document ID (Org No.):

2001357020

pISSN:

2458-8806

Antihypertension

Lipid-polymeric nanovesicles

Valsartan

Bioavailability

Sayı

Makale detayları

Formulation and evaluation of lipid–polymeric hybrid nanovesicles for valsartan delivery: Bridging in vitro and in vivo Pharmacokinetics

Yazarlar: Sayani Bhattacharyya | Maithili Sinha | Sweta Jha

Yayıncı: Hacettepe University

Ana Başlıklar: Pharmaceutical Sciences | Pharmaceutical Delivery Technologies

Dergi: Hacettepe University Journal of the Faculty of Pharmacy Vol.45 Issue 3, pp.211-222

Belge Tipi: Makale

Yayın Tarihi: 1/2025

Belge Dili: İngilizce

Document ID (Org No.): 2001357020

pISSN: 2458-8806

Antihypertension

Lipid-polymeric nanovesicles

Valsartan

Bioavailability

Sayı

Yazarlar:

Sayani Bhattacharyya | Maithili Sinha | Sweta Jha

Yayıncı:

Hacettepe University

Ana Başlıklar:

Pharmaceutical Sciences | Pharmaceutical Delivery Technologies

Dergi:

Hacettepe University Journal of the Faculty of Pharmacy Vol.45 Issue 3, pp.211-222

Belge Tipi:

Makale

Yayın Tarihi:

1/2025

Belge Dili:

İngilizce

Document ID (Org No.):

2001357020

pISSN:

2458-8806