Novel semisolid SNEDDS based on PEG-30-di-(polyhydroxystearate): Progesterone incorporation and in vitro digestion

Hassan, Tamer H.; Mäder, Karsten

doi:10.1016/j.ijpharm.2015.03.044

Cited by 12 publications

(3 citation statements)

References 43 publications

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“…There are various articles in the literature regarding this. Solid surfactants such as Cithrol ® DPHS [ 41 ], Gelucire ® 44/14 [ 42 , 43 ], Gelucire ® 48/16 [ 44 , 45 ], and poloxamer 188 [ 46 ] were used for this purpose. Problems such as leakage can occur when filling liquid SNEDDS formulations directly into capsules [ 47 ].…”

Section: Resultsmentioning

confidence: 99%

A Novel Semi-Solid Self-Emulsifying Formulation of Aprepitant for Oral Delivery: An In Vitro Evaluation

et al. 2023

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Aprepitant is the first member of a relatively new antiemetic drug class called NK1 receptor antagonists. It is commonly prescribed to prevent chemotherapy-induced nausea and vomiting. Although it is included in many treatment guidelines, its poor solubility causes bioavailability issues. A particle size reduction technique was used in the commercial formulation to overcome low bioavailability. Production with this method consists of many successive steps that cause the cost of the drug to increase. This study aims to develop an alternative, cost-effective formulation to the existing nanocrystal form. We designed a self-emulsifying formulation that can be filled into capsules in a melted state and then solidified at room temperature. Solidification was achieved by using surfactants with a melting temperature above room temperature. Various polymers have also been tested to maintain the supersaturated state of the drug. The optimized formulation consists of CapryolTM 90, Kolliphor® CS20, Transcutol® P, and Soluplus®; it was characterized by DLS, FTIR, DSC, and XRPD techniques. A lipolysis test was conducted to predict the digestion performance of formulations in the gastrointestinal system. Dissolution studies showed an increased dissolution rate of the drug. Finally, the cytotoxicity of the formulation was tested in the Caco-2 cell line. According to the results, a formulation with improved solubility and low toxicity was obtained.

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Section: Resultsmentioning

confidence: 99%

A Novel Semi-Solid Self-Emulsifying Formulation of Aprepitant for Oral Delivery: An In Vitro Evaluation

et al. 2023

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“…PEG-30 dipolyhydroxystearate (Cithrol DPHS from Croda International plc, Snaith, UK) was used as molecular stabiliser based on reports about its capability to form stable W/O emulsions in triolein and other oils and contributions that centre around its applicability for oral drug delivery [ 131 , 132 ]. Its chemical structure is shown in Figure 3 .…”

Section: Methodsmentioning

confidence: 99%

Inverse ISAsomes in Bio-Compatible Oils—Exploring Formulations in Squalane, Triolein and Olive Oil

2022

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In contrast to their more common counterparts in aqueous solutions, inverse ISAsomes (internally self-assembled somes/particles) are formulated as kinetically stabilised dispersions of hydrophilic, lyotropic liquid-crystalline (LC) phases in non-polar oils. This contribution reports on their formation in bio-compatible oils. We found that it is possible to create inverse hexosomes, inverse micellar cubosomes (Fd3m) and an inverse emulsified microemulsion (EME) in excess squalane with a polyethylene glycol alkyl ether as the primary surfactant forming the LC phase and to stabilise them with hydrophobised silica nanoparticles. Furthermore, an emulsified -phase and inverse hexosomes were formed in excess triolein with the triblock-copolymer Pluronic® P94 as the primary surfactant. Stabilisation was achieved with a molecular stabiliser of type polyethylene glycol (PEG)-dipolyhydroxystearate. For the inverse hexosomes in triolein, the possibility of a formulation without any additional stabiliser was explored. It was found that a sufficiently strong stabilisation effect was created by the primary surfactant alone. Finally, triolein was replaced with olive oil which also led to the successful formation of inverse hexosomes. As far as we know, there exists no previous contribution about inverse ISAsomes in complex oils such as triolein or plant oils, and the existence of stabiliser-free (i.e., self-stabilising) inverse hexosomes has also not been reported until now.

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“…It was also observed that PG remained in the solubilized form in lipids without getting crystallized. Thus, PEG-30-di-(polyhydroxystearate) (Cithrol DPHS) containing SNEDDS are essential for developing bio robust therapeutic systems [50]. Apart from oral delivery, scientists had also focussed upon other routes of delivery as well.…”

Section: The Panorama Of Novel Progesteronementioning

confidence: 99%

Nanonized progesterone formulation for improved oral bioavailability in healthy and pregnant rabbits

Jain¹,

Sharma²,

Modi³

et al. 2022

Journal of Pharmaceutical Negative Results

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The aim of this study is to evaluate and compare the oral bioavailability of nanonized progesterone (nano-PG) and micronized progesterone (micro-PG) sustained release tablet formulation in healthy and pregnant rabbits. High pressure compressed gas technology reduces the particle size from 1.72 ± 2.5 μm (micro-PG) to 800 ± 35 nm (nano-PG). DSC and XRD showed that both micro-PG and nano-PG were crystalline and exist as form I. Higher melting enthalpy of nano-PG indicated improved drug stability whereas XRD showed slight reduction in degree of crystallanity following nanonization. Nano-PG demonstrated 2-fold higher solubility in SDS aqueous solution and significantly higher permeability (p < 0.05) across porcine intestine compared to micro-PG. The pharmacokinetics of nano-PG and micro-PG was conducted in healthy and pregnant rabbits. The Cmax of nano-PG was higher in healthy and pregnant rabbits however the difference was significant in healthy rabbits only. The nano-PG demonstrated 30% and 18% higher bioavailability compared to micro-PG in healthy and pregnant rabbits, respectively. In conclusion, nanonization improves solubility, dissolution and bioavailability of PG in rabbits without affecting solid state characters.

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Novel semisolid SNEDDS based on PEG-30-di-(polyhydroxystearate): Progesterone incorporation and in vitro digestion

Cited by 12 publications

References 43 publications

A Novel Semi-Solid Self-Emulsifying Formulation of Aprepitant for Oral Delivery: An In Vitro Evaluation

A Novel Semi-Solid Self-Emulsifying Formulation of Aprepitant for Oral Delivery: An In Vitro Evaluation

Inverse ISAsomes in Bio-Compatible Oils—Exploring Formulations in Squalane, Triolein and Olive Oil

Nanonized progesterone formulation for improved oral bioavailability in healthy and pregnant rabbits

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