A New Long-Acting Injectable Microcapsule System for the Administration of Progesterone

Beck, Lee R.; Cowsar, Donald R.; Lewis, Danny; Cosgrove, Robert; Riddle, Charles T.; Lowry, Suzanne L.; Epperly, T

doi:10.1016/s0015-0282(16)44002-1

Cited by 205 publications

(33 citation statements)

References 6 publications

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“…The importance of natural progesterone arises from its similarity to the progesterone naturally present in high concentrations in the body and therefore does not pose any toxicity problems, unlike synthetic progesterone. 25,26 Progesterone is not orally active except in high doses and has a very short biological half life, which makes it an ideal candidate for inclusion in a thermosensitive matrix which controls its deposition and sustains its action when given by the IM route of administration. Hydrophobicity, low solubility, and the large particle size of natural progesterone hinder its uniform distribution in hydrophilic thermosensitive polymers.…”

Section: Resultsmentioning

confidence: 99%

Sustained-release progesterone nanosuspension following intramuscular injection in ovariectomized rats

Salem¹

2010

IJN

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Abstract:The production of an intramuscular (IM) injection of natural progesterone would provide a safer solution than using semi synthetic progesterone. However, disadvantages such as low solubility and a short half life prevent the use of natural progesterone. In this study, we formulated a sustained release form of natural progesterone to be given as IM injection. A progesterone nanosuspension (PNS) was first developed and then dispersed in a thermosensitive gel matrix. The selected nanoparticles showed an average particle size of 267 nm and a zeta potential approaching-41 mV. The in vitro release profile of PNS from the F127 plus methyl cellulose gel followed zero order kinetics and correlated linearly with the weight percentage of gel dissolved, demonstrating that the overall rate of release of PNS is controlled by dissolution of the pluronic F127/methyl cellulose (MC) gel (r 2 . 0.99). The pharmacokinetic parameters of the PNS (6 mg/mL) in pluronic F127/MC gel were evaluated in comparison with the control progesterone suspension. After the administration of PNS in F127/MC gel into the rats, a maximum serum concentration of 22.1 ± 1.9 ng/mL was reached at a T max of 4.05 ± 0.1 h. The terminal half life was 12.7 ± 0.8 h. The area under the curve AUC 0-∞ of the injected formula was 452.75 ± 42.8 ng·h/mL and the total mean residence time was 18.57 ± 1.44 h. The PNS in gel was significantly different from the control in rate and extent at P , 0.001. The natural progesterone which was nanosized and formulated in a thermosensitive gel significantly sustained the action of natural progesterone so that it could be injected every 36 h instead of every day. Moreover, this formula is expected to provide a much safer choice than the use of semi-synthetic progesterone.

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Section: Resultsmentioning

confidence: 99%

Sustained-release progesterone nanosuspension following intramuscular injection in ovariectomized rats

Salem¹

2010

IJN

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“…3 One of the widely investigated methods for microencapsulation of drugs is the oil-in-water emulsion-solvent evaporation (ESE) technique. 4 The characteristics of the microcapsules such as drug entrapment efficiency and release of drug, however, depend on the aqueous solubility of the drug, the type of organic solvent or solvent mixture used, the phase ratio of the emulsion system, the temperature, and the type and concentration of emulsion stabilizers. 5 The encapsulation efficiency of water-soluble drugs, in particular, by the oil-in-water ESE method has been low because of partitioning of drugs from the organic phase to the external aqueous phase.…”

Section: Introductionmentioning

confidence: 99%

Preparation and in vitro evaluation of polystyrene-coated diltiazem-resin complex by oil-in-water emulsion solvent evaporation method

Halder

2006

AAPS PharmSciTech

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The purpose of this study was to examine the suitability of polystyrene-coated (PS-coated) microcapsules of drug-resin complex for achieving prolonged release of diltiazem-HCl, a highly water-soluble drug, in simulated gastric and intestinal fluid. The drug was bound to Indion 254, a cation-exchange resin, and the resulting resinate was microencapsulated with PS using an oil-in-water emulsion-solvent evaporation method. The effect of various formulation parameters on the characteristics of the microcapsules was studied. Mean diameter and encapsulation efficiency of the microcapsules rose with an increase in the concentration of emulsion stabilizer and the coat/core ratio, while the same characteristics tended to decrease with an increase in the volume of the organic disperse phase. The desorption of drug from the uncoated resinate was quite rapid and independent of the pH of the dissolution media. On the other hand, the drug release from the microcapsules was prolonged for different periods of time depending on the formulation parameters and was also found to be independent of the pH of the dissolution media. Both the encapsulation efficiency and the retardation of drug release were found to be dependent on the uniformity of coating, which in turn was influenced by the formulation parameters. Kinetic studies revealed that the desorption of drug from the resinate obeyed the typical particle diffusion process, whereas the drug release from the microencapsulated resinate followed the diffusioncontrolled model in accordance with the Higuchi equation. PS appeared to be a suitable polymer to provide prolonged release of diltiazem independent of the pH of the dissolution media.

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“…Controlled drug delivery systems in comparison to immediate drug delivery systems offer desired concentration of drugs at the absorption site allowing maintenance of drug concentration within the therapeutic range, lowering frequency of drug administration and thus, enhancing patient compliance (Wahab et al, 2011). The emulsion solvent evaporation method may be employed to prepare microcapsules of water insoluble drugs within water insoluble polymers (Beck et al, 1979).…”

Section: Ibuprofen (Ibn) Is a Non-steroidal Anti-inflammatory Drugmentioning

confidence: 99%

Novel modified release tableted microspheres of ibuprofen and misoprostol in a combined formulation: Use of software DDSolver

Akhtar

Ahmad²,

Khan³

et al. 2012

Afr. J. Pharm. Pharmacol.

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The current study was aimed to develop a stable sustained release drug delivery system for ibuprofen and a cytoprotective agent misoprostol in a combined dosage form. Non-aqueous emulsion solvent evaporation method was used to prepare ibuprofen microspheres. Ethylcellulose (EC) and Hydroxypropyl methylcellulose (HPMC) were used as the release retarding polymers in combination. Ibuprofen microspheres were prepared separately and then compressed into tablet dosage forms with misoprostol dispersions in HPMC. For surface topography of microspheres, Scanning Electron Microscope (SEM) was used. Fourier transformed infrared (FTIR) spectroscopy and X-ray diffractometry (XRD) were employed to evaluate pharmaceutical incompatibility and physical state of drug in formulation. The mechanism and pattern of drug release were determined by applying kinetic models. Tableted microspheres were also assessed for accelerated stability study for three months. SEM showed spherical shape microspheres. FTIR and XRD data for developed formulation indicated stability and compatibility of drugs with excipients. After 10 h, 86.97 and 89.33% of ibuprofen and misoprostol were released from micro particles while 75.43 and 77.65% from tableted microspheres, respectively. Non-aqueous emulsion solvent evaporation was found to be a suitable method to prepare stable sustained release tableted microspheres of ibuprofen and misoprostol in combination.

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A New Long-Acting Injectable Microcapsule System for the Administration of Progesterone

Cited by 205 publications

References 6 publications

Sustained-release progesterone nanosuspension following intramuscular injection in ovariectomized rats

Sustained-release progesterone nanosuspension following intramuscular injection in ovariectomized rats

Preparation and in vitro evaluation of polystyrene-coated diltiazem-resin complex by oil-in-water emulsion solvent evaporation method

Novel modified release tableted microspheres of ibuprofen and misoprostol in a combined formulation: Use of software DDSolver

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