Display options
Cite
Brewster ME, Estes KS, Bodor N. Improved Delivery Through Biological Membranes. XXIV. Synthesis, in Vitro Studies, and in Vivo Characterization of Brain-Specific and Sustained Progestin Delivery Systems. Pharm Res. 1986;3(5):278-85doi: 10.1023/A:1016359301852.
Brewster, M. E., Estes, K. S., & Bodor, N. (1986). Improved Delivery Through Biological Membranes. XXIV. Synthesis, in Vitro Studies, and in Vivo Characterization of Brain-Specific and Sustained Progestin Delivery Systems. Pharmaceutical research, 3(5), 278-85. https://doi.org/10.1023/A:1016359301852
Brewster, M E, et al. "Improved Delivery Through Biological Membranes. XXIV. Synthesis, in Vitro Studies, and in Vivo Characterization of Brain-Specific and Sustained Progestin Delivery Systems." Pharmaceutical research vol. 3,5 (1986): 278-85. doi: https://doi.org/10.1023/A:1016359301852
Brewster ME, Estes KS, Bodor N. Improved Delivery Through Biological Membranes. XXIV. Synthesis, in Vitro Studies, and in Vivo Characterization of Brain-Specific and Sustained Progestin Delivery Systems. Pharm Res. 1986 Oct;3(5):278-85. doi: 10.1023/A:1016359301852. PMID: 24271710.
Copy Download .nbib Format: NLM
Share it on

Pharm Res. 1986 Oct;3(5):278-85. doi: 10.1023/A:1016359301852.

Improved Delivery Through Biological Membranes. XXIV. Synthesis, in Vitro Studies, and in Vivo Characterization of Brain-Specific and Sustained Progestin Delivery Systems.

Pharmaceutical research

M E Brewster, K S Estes, N Bodor

Affiliations

  1. Pharmatec, Inc, 730, Alachua, Florida, 32615.

PMID: 24271710 DOI: 10.1023/A:1016359301852

Abstract

Dihydropyridine ⇄ pyridinium salt-based brain-selective delivery systems were synthesized for the progestins, ethisterone, norethindrone, and norgestrel. After initial lipophilicity and in vitro studies indicated the feasibility of applying these compounds to brain-specific delivery, in vivo distribution studies were performed on one of the redox delivery systems. After systemic administration of the chemical delivery system based on norethindrone, sustained and selective delivery of the oxidized form of the drug-carrier complex was observed in the brain. In addition, a slow and sustained release of the parent steroid, norethindrone, occurred. This release produced substantially higher levels of norethindrone for more prolonged periods than the administration of norethindrone itself.

References

  1. Pharmacol Ther. 1982;19(3):337-86 - PubMed
  2. J Pharm Sci. 1984 Mar;73(3):385-9 - PubMed
  3. Science. 1981 Dec 18;214(4527):1370-2 - PubMed
  4. Am J Obstet Gynecol. 1977 May 1;128(1):60-74 - PubMed
  5. J Pharm Sci. 1977 May;66(5):747-9 - PubMed

Publication Types