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Mechanism of enhanced oral absorption of hydrophilic drug incorporated in hydrophobic nanoparticles.

Lv LZ, Tong CQ, Yu J, Han M, Gao JQ - Int J Nanomedicine (2013)

Bottom Line: Hydroxysafflor yellow A (HSYA) is an effective ingredient of the Chinese herb Carthamus tinctorius L, which has high water solubility and low oral bioavailability.This research aims to develop a hydrophobic nanoparticle that can enhance the oral absorption of HSYA.Both enhanced uptake in Caco-2 cells monolayer and increased bioavailability in rats for HSYA nanoparticles indicated that the formulation could improve bioavailability of HSYA significantly after oral administration both in vitro and in vivo.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmacy, Zhejiang Provincial People's Hospital, Hangzhou, People's Republic of China.

ABSTRACT
Hydroxysafflor yellow A (HSYA) is an effective ingredient of the Chinese herb Carthamus tinctorius L, which has high water solubility and low oral bioavailability. This research aims to develop a hydrophobic nanoparticle that can enhance the oral absorption of HSYA. Transmission electron microscopy and freeze-fracture replication transmission election microscopy showed that the HSYA nanoparticles have an irregular shape and a narrow size distribution. Zonula occludens 1 protein (ZO-1) labeling showed that the nanoparticles with different dilutions produced an opening in the tight junctions of Caco-2 cells without inducing cytotoxicity to the cells. Both enhanced uptake in Caco-2 cells monolayer and increased bioavailability in rats for HSYA nanoparticles indicated that the formulation could improve bioavailability of HSYA significantly after oral administration both in vitro and in vivo.

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(A) Plasma concentration-time profiles of HSYA after intravenous administration of HSYA solution, (B) oral administration of HSYA solution, and (C) HSYA-NPs to rats at a dose of 25 mg/kg.Abbreviations: HSYA, hydroxysafflor yellow A; NP, nanoparticle.
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f6-ijn-8-2709: (A) Plasma concentration-time profiles of HSYA after intravenous administration of HSYA solution, (B) oral administration of HSYA solution, and (C) HSYA-NPs to rats at a dose of 25 mg/kg.Abbreviations: HSYA, hydroxysafflor yellow A; NP, nanoparticle.

Mentions: The plasma concentration-time profiles of HSYA after intravenous or oral administration of HSYA solution and HSYA nanoparticles to rats are shown in Figure 6, and the pharmacokinetic parameters are summarized in Table 1. The AUC of HSYA nanoparticles was 23.3-fold greater than that of the HSYA solution.


Mechanism of enhanced oral absorption of hydrophilic drug incorporated in hydrophobic nanoparticles.

Lv LZ, Tong CQ, Yu J, Han M, Gao JQ - Int J Nanomedicine (2013)

(A) Plasma concentration-time profiles of HSYA after intravenous administration of HSYA solution, (B) oral administration of HSYA solution, and (C) HSYA-NPs to rats at a dose of 25 mg/kg.Abbreviations: HSYA, hydroxysafflor yellow A; NP, nanoparticle.
© Copyright Policy
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC3735274&req=5

f6-ijn-8-2709: (A) Plasma concentration-time profiles of HSYA after intravenous administration of HSYA solution, (B) oral administration of HSYA solution, and (C) HSYA-NPs to rats at a dose of 25 mg/kg.Abbreviations: HSYA, hydroxysafflor yellow A; NP, nanoparticle.
Mentions: The plasma concentration-time profiles of HSYA after intravenous or oral administration of HSYA solution and HSYA nanoparticles to rats are shown in Figure 6, and the pharmacokinetic parameters are summarized in Table 1. The AUC of HSYA nanoparticles was 23.3-fold greater than that of the HSYA solution.

Bottom Line: Hydroxysafflor yellow A (HSYA) is an effective ingredient of the Chinese herb Carthamus tinctorius L, which has high water solubility and low oral bioavailability.This research aims to develop a hydrophobic nanoparticle that can enhance the oral absorption of HSYA.Both enhanced uptake in Caco-2 cells monolayer and increased bioavailability in rats for HSYA nanoparticles indicated that the formulation could improve bioavailability of HSYA significantly after oral administration both in vitro and in vivo.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmacy, Zhejiang Provincial People's Hospital, Hangzhou, People's Republic of China.

ABSTRACT
Hydroxysafflor yellow A (HSYA) is an effective ingredient of the Chinese herb Carthamus tinctorius L, which has high water solubility and low oral bioavailability. This research aims to develop a hydrophobic nanoparticle that can enhance the oral absorption of HSYA. Transmission electron microscopy and freeze-fracture replication transmission election microscopy showed that the HSYA nanoparticles have an irregular shape and a narrow size distribution. Zonula occludens 1 protein (ZO-1) labeling showed that the nanoparticles with different dilutions produced an opening in the tight junctions of Caco-2 cells without inducing cytotoxicity to the cells. Both enhanced uptake in Caco-2 cells monolayer and increased bioavailability in rats for HSYA nanoparticles indicated that the formulation could improve bioavailability of HSYA significantly after oral administration both in vitro and in vivo.

Show MeSH
Related in: MedlinePlus