In Vivo Release of Norethindrone Coupled to a Biodegradable Poly(α-amino acid) Drug Delivery System

Zupon, M.A.; Fang, Sen-Maw; Christensen, J. Mark; Petersen, Robert V.

doi:10.1002/jps.2600721121

Cited by 16 publications

(9 citation statements)

References 16 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…41 The contraceptive norethindrone was attached via a 17-carbonate linkage to poly-JV 5 -(3-hydroxypropyl)-L-glutamine. In rats the contraceptive agent was slowly released over a 9-month period.…”

Section: 34mentioning

confidence: 99%

Prodrugs and Drug Delivery Systems

Silverman

1992

The Organic Chemistry of Drug Design and Drug Action

View full text Add to dashboard Cite

Section: 34mentioning

confidence: 99%

Prodrugs and Drug Delivery Systems

Silverman

1992

The Organic Chemistry of Drug Design and Drug Action

View full text Add to dashboard Cite

“…Some pharmaceutical formulations, for example, use amphiphilic excipients, comprised of hydrophobic and hydrophilic blocks, to form micelles that solubilize hydrophobic drugs in aqueous environments, thus improving their bioavailability. 6, 15–20 …”

mentioning

confidence: 99%

Antitumor Activity of Peptide Amphiphile Nanofiber-Encapsulated Camptothecin

et al. 2011

View full text Add to dashboard Cite

Self-assembling peptide amphiphile (PA) nanofibers were used to encapsulate camptothecin (CPT), a naturally occurring hydrophobic chemotherapy agent, using a solvent evaporation technique. Encapsulation by PA nanofibers was found to improve the aqueous solubility of the CPT molecule by more than 50-fold. PAs self-assembled into nanofibers in the presence of CPT as demonstrated by transmission electron microscopy. Small-angle X-ray scattering results suggest a slight increase in diameter of the nanofiber to accommodate the hydrophobic cargo. In vitro studies using human breast cancer cells show an enhancement in antitumor activity of the CPT when encapsulated by the PA nanofibers. In addition, using a mouse orthotopic model of human breast cancer, treatment with PA nanofiber encapsulated CPT inhibited tumor growth. These results highlight the potential of this model PA system to be adapted for delivery of hydrophobic therapies to treat a variety of diseases including cancer.

show abstract

“…The concentration was maintained up to 120 days, and only 10% of NET had been release from PHBA. These concentration levels have already been demonstrated to be in the therapeutic level (18). An initial high concentration spike also appeared.…”

Section: In Vivo Release Studymentioning

confidence: 64%

Controlled Delivery System for Norethindrone Based on Biodegradable Poly- α, β -(Hydroxyalkyl)-DL-Aspartamide

Tang

Zhu²,

Chen³

2002

Drug Delivery

View full text Add to dashboard Cite

The article describes the preparation of poly-(hydroxyalkyl)-DL-aspartamide (PHAA) by a (ring) opening reaction by hydroxyalkylamino; norethindrone (NET), as a model drug, was coupled to the polymers via hydroxyalkylamino spacers. PHAA and NETPHAA conjugates were characterized by FTIR, DSC, x-ray,(13)C NMR, and scanning electron microscopy and their structure were confirmed. The biocompatibility of PHAA was tested. The study showed that PHAA was a hydrophilic, nontoxic in vivo, nonantigenic material and had good biocompatibility as a drug carrier. The effect on drug release from the polymer of length of side chain, initial drug loading, and particle size of the polymer drug were investigated in tris-HCl buffer solution (pH 7.4, t = 37 degrees C). In vivo release in rabbits also was performed for 120 days. The experiment indicated that the concentration of NET in rabbits can be 1-2 microg/ml serum after 1 month; 10% of NET had been released from the polymer.

show abstract

In Vivo Release of Norethindrone Coupled to a Biodegradable Poly(α-amino acid) Drug Delivery System

Cited by 16 publications

References 16 publications

Prodrugs and Drug Delivery Systems

Prodrugs and Drug Delivery Systems

Antitumor Activity of Peptide Amphiphile Nanofiber-Encapsulated Camptothecin

Controlled Delivery System for Norethindrone Based on Biodegradable Poly- α, β -(Hydroxyalkyl)-DL-Aspartamide

Contact Info

Product

Resources

About