Endometrin®/prometrium® versus intramuscular progesterone administration for luteal phase support

Sabouni, Reem; Williams, Daniel B.; Griffith, Jason; Haddad, Ghassan; Witz, Craig A.

doi:10.1016/j.fertnstert.2015.12.097

Cited by 1 publication

(2 citation statements)

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“…15 Currently, PG is administrated via intramuscular injection to assure reliable absorption, but the oil dispersions in PG oil-based injection (PG/OI) often accumulate in the injection sites and further cause painful and inflamed side effects after long-term injection. 16,17 Herein, we provide an easy and effective one-shot method to produce water-based drug nanocrystal suspension injection with the desired nanoscale size in an aseptic condition by a "bottom-up" technology (Scheme 1). First, the nanocrystals were prepared by freeze-drying PG oil in water (O/W) emulsions, which are composed of water, dichloromethane (DCM), and n-butanol, into nanocrystal powders.…”

Section: Introductionmentioning

confidence: 99%

“…It also plays an important role in brain function and intermediates the production of other steroids. , However, the solubility of PG is 16 μg/mL in distilled water at 25°C, and the poor solubility and low permeability result in very low absorption and bioavailability . Currently, PG is administrated via intramuscular injection to assure reliable absorption, but the oil dispersions in PG oil-based injection (PG/OI) often accumulate in the injection sites and further cause painful and inflamed side effects after long-term injection. , …”

Section: Introductionmentioning

confidence: 99%

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An Aseptic One-Shot Bottom-Up Method To Produce Progesterone Nanocrystals: Controlled Size and Improved Bioavailability

Zhai

et al. 2019

Mol. Pharmaceutics

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Progesterone (PG) is an essential sex hormone with a variety of important biological functions, but its insolubility leads to low bioavailability of most water-based formulations. What is more, the commercial oil-based formulations often cause severe side effects after long-term injection due to poor tissue absorption of oil. Herein, we report an aseptic bottom-up method utilizing emulsion freeze-drying technology that produces size-controllable, highly bioavailable, and water-based PG nanocrystal injection. The key factors that can determine the features of nanocrystals were investigated, including solvents, water-to-oil ratio, drug concentrations, type of surfactants, temperature in freeze-drying process, and lyoprotectants. Mechanisms of crystal growth formation process for PG nanocrystals were also analyzed theoretically. The prepared water-based PG nanocrystal suspension injection (PG/NSI) not only showed quick dissolution behaviors but also had significantly improved bioavailability in vivo. Therefore, this method can effectively control the size of nanocrystals, enhance bioavailability of insoluble drugs, and produce aseptic water-based nanocrystals that can be directly used for injection. Moreover, this method can also be used to prepare nanocrystals with the desired size under aseptic conditions for other poorly water-soluble drugs.

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Section: Introductionmentioning

confidence: 99%