Nanomedicine for uterine leiomyoma therapy.
BACKGROUND
The purpose of this work was to engineer polymeric nanoparticles to encapsulate and deliver 2-methoxyestradiol, a potential antitumor drug for treatment of uterine leiomyoma (fibroids), the most common hormone-dependent pathology affecting women of reproductive age.


RESULTS
Encapsulation efficiency and drug release from the nanoparticles were monitored by HPLC. Cell morphology and in vitro cytotoxicity experiments were carried out in a human leiomyoma cell line. The nanoparticles displayed high encapsulation efficiency (>86%), which was verified by differential scanning calorimetry and x-ray diffraction. Excellent long-term stability of the nanoparticles and gradual drug release without burst were also observed. Cellular uptake of fluorescent nanoparticles was confirmed by confocal imaging. The drug-loaded poly(lactic acid) and poly(lactic-co-glycolic acid) nanoparticles induced cytotoxicity in human leiomyoma cells to a significantly greater extent than the free drug at 0.35 µM.


CONCLUSIONS
This novel approach represents a potential fertility-preserving alternative to hysterectomy.
Department of Obstetrics & Gynecology, University of Texas Medical Branch, Galveston, TX 77555, USA.
Hazem
H
Ali
Gokhan
G
Kilic
Kathleen
K
Vincent
Massoud
M
Motamedi
Erik
E
Rytting
D000077584:2-Methoxyestradiol; D002152:Calorimetry, Differential Scanning; D045744:Cell Line, Tumor; D002851:Chromatography, High Pressure Liquid; D004337:Drug Carriers / Q000737:chemistry; D004355:Drug Stability; D004356:Drug Storage; D004958:Estradiol / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000493:pharmacokinetics / Q000494:pharmacology; D005260:Female; D006801:Humans; D019344:Lactic Acid / Q000737:chemistry; D007889:Leiomyoma / Q000188:drug therapy* / Q000473:pathology; D050997:Nanomedicine / Q000379:methods; D053758:Nanoparticles; D011091:Polyesters; D011100:Polyglycolic Acid / Q000737:chemistry; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011108:Polymers / Q000737:chemistry; D013997:Time Factors; D050257:Tubulin Modulators / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology; D014594:Uterine Neoplasms / Q000188:drug therapy* / Q000473:pathology; D014961:X-Ray Diffraction
D004337:Drug Carriers; D011091:Polyesters; D011108:Polymers; D050257:Tubulin Modulators; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; C033616:poly(lactide); D004958:Estradiol; D000077584:2-Methoxyestradiol