Bioavailability of seocalcitol

Grove, Mette; Müllertz, Anette; Nielsen, Jeanet L.; Pedersen, Gitte Pommergaard

doi:10.1016/j.ejps.2006.02.005

Cited by 101 publications

(15 citation statements)

References 28 publications

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“…As the more hydrophobic LCT is more difficult to emulsify, higher concentration of Cremophor ® RH 40 was generally required to form microemulsions when using LCT compared to MCT. Nevertheless, no significant differences were observed in the absorption and bioavailability of seocalcitol between the two aforemen- tioned SMEDDS upon their oral administration to male rats (28). This is contrary to previous studies, where the bioavailability of danazol and halofantrine from SMEDDS containing LCT was found to be superior to SMEDDS containing MCT (22,29).…”

Section: Chemism Of Lipidscontrasting

confidence: 55%

“…Otherwise, derivatives of ethylene-glycol, glycerol, and propylene glycol can be also included (11,16,34). When choosing between co-solvent and co-surfactant, one should consider lower solubilization capacity for hydrophobic drugs observed upon diluting co-solvent-containing formulations with the aqueous phase (28). This is related to the large amount of co-solvent usually needed to improve the drug solubilization capacity, which in turn increases the risk of drug precipitation when the formulation is dispersed in aqueous media.…”

Section: Chemism Of Lipidsmentioning

confidence: 99%

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Lipid-based systems as a promising approach for enhancing the bioavailability of poorly water-soluble drugs

Čerpnjak¹,

Zvonar²,

Gašperlin³

et al. 2013

Acta Pharmaceutica

185

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Low oral bioavailability as a consequence of low water solubility of drugs is a growing challenge to the development of new pharmaceutical products. One of the most popular approaches of oral bioavailability and solubility enhancement is the utilization of lipid-based drug delivery systems. Their use in product development is growing due to the versatility of pharmaceutical lipid excipients and drug formulations, and their compatibility with liquid, semi-solid, and solid dosage forms. Lipid formulations, such as self-emulsifying (SEDDS), self-microemulsifying SMEDDS) and self--nanoemulsifying drug delivery systems (SNEDDS) were explored in many studies as an efficient approach for improving the bioavailability and dissolution rate of poorly water-soluble drugs. One of the greatest advantages of incorporating poorly soluble drugs into such formulations is their spontaneous emulsification and formation of an emulsion, microemulsion or nanoemulsion in aqueous media. This review article focuses on the following topics. First, it presents a classification overview of lipid-based drug delivery systems and mechanisms involved in improving the solubility and bioavailability of poorly water-soluble drugs. Second, the article reviews components of lipid-based drug delivery systems for oral use with their characteristics. Third, it brings a detailed description of SEDDS, SMEDDS and SNEDDS, which are very often misused in literature, with special emphasis on the comparison between microemulsions and nanoemulsions.Keywords: lipid-based drug delivery systems (LBDDS), self-emulsifying drug delivery systems (SEDDS), self--microemulsifying drug delivery systems (SMEDDS), self-nanoemulsifying drug delivery systems (SNEDDS), microemulsions, nanoemulsions

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Section: Chemism Of Lipidscontrasting

confidence: 55%

Section: Chemism Of Lipidsmentioning

confidence: 99%

Lipid-based systems as a promising approach for enhancing the bioavailability of poorly water-soluble drugs

Čerpnjak¹,

Zvonar²,

Gašperlin³

et al. 2013

Acta Pharmaceutica

185

View full text Add to dashboard Cite

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“…Precisely, a fixed ratio of 10% of the oil was employed as recommended to produce spontaneous L-SEDDs formulations with small DS upon dispersion [28]. Based on the literature review, many reports showed that drugs' solubilities in various oils and surfactants might vary based on the carbon chain lengths of the oils and surfactants [81], including MCT [82][83][84], and LCT [85,86]. This attitude is probably linked to the employed drug physicochemical properties [82,87].…”

Section: Emulsification Efficiency Studiesmentioning

confidence: 99%

Liquid and Solid Self-Emulsifying Drug Delivery Systems (SEDDs) as Carriers for the Oral Delivery of Azithromycin: Optimization, In Vitro Characterization and Stability Assessment

et al. 2020

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Azithromycin (AZM) is a macrolide antibiotic used for the treatment of various bacterial infections. The drug is known to have low oral bioavailability (37%) which may be attributed to its relatively high molecular weight, low solubility, dissolution rate, and incomplete intestinal absorption. To overcome these drawbacks, liquid (L) and solid (S) self-emulsifying drug delivery systems (SEDDs) of AZM were developed and optimized. Eight different pseudo-ternary diagrams were constructed based on the drug solubility and the emulsification studies in various SEDDs excipients at different surfactant to co-surfactant (Smix) ratios. Droplet size (DS) < 150 nm, dispersity (Đ) ≤ 0.7, and transmittance (T)% > 85 in three diluents of distilled water (DW), 0.1 mM HCl, and simulated intestinal fluids (SIF) were considered as the selection criteria. The final formulations of L-SEDDs (L-F1(H)), and S-SEDDs (S-F1(H)) were able to meet the selection requirements. Both formulations were proven to be cytocompatible and able to open up the cellular epithelial tight junctions (TJ). The drug dissolution studies showed that after 5 min > 90% and 52.22% of the AZM was released from liquid and solid SEDDs formulations in DW, respectively, compared to 11.27% of the pure AZM, suggesting the developed SEDDs may enhance the oral delivery of the drug. The formulations were stable at refrigerator storage conditions.

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“…As the more hydrophobic LCT is more difficult to emulsify, higher concentration of Cremophor® RH 40 was generally required to form microemulsions when using LCT compared to MCT. Nevertheless, no significant differences were observed in the absorption and bioavailability of seocalcitol between the two aforementioned SMEDDS upon their oral administration to male rats 37 . This is contrary to previous studies, where the bioavailability of danazol and halofantrine from SMEDDS containing LCT was found to be superior compared to SMEDDS containing MCT 38,39 .…”

Section: Medium Chain Triglycerides (Mct) and Related Estersmentioning

confidence: 85%

“…However, SMEDDS compared in these studies consisted of different amounts of lipid and surfactant, whereas Grovea et al used quantitatively comparable systems. Considering the mentioned data, one can conclude that the extent of influence of MCT and LCT on the bioavailability of drugs is drug specific 37 .…”

Section: Medium Chain Triglycerides (Mct) and Related Estersmentioning

confidence: 95%

Self-Micro Emulsifying Drug Delivery Systems (Smedds): A Review on Physico-Chemical and Biopharmaceutical Aspects

Maurya

Arya

Rajpal

et al. 2017

J. Drug Delivery Ther.

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Cite this article as:Maurya SD, Arya RKK, Rajpal G, Dhakar RC, Self-micro emulsifying drug delivery systems (SMEDDS): a review on physico-chemical and biopharmaceutical aspects, Journal of Drug Delivery and Therapeutics. 2017; 7(3):55-65 DOI: http://dx. ABSTRACTNearly 40% of new drug candidates exhibit low solubility in water, which is a challenge in development of optimum oral solid dosage form in terms of formulation design and bioavailability of new pharmaceutical products. Many strategies have been used to overcome these problems either by means of modifying the solubility or maintaining the drug in dissolved form throughout gastric transit time. Much attention has focused on lipid solutions, emulsions and emulsion pre-concentrates, which can be prepared as physically stable formulations suitable for encapsulation of such poorly soluble drugs. Recently, self-micro emulsifying drug delivery systems (SMEDDS) especially have attracted increasing interest primarily because these are physically stable, easy to manufacture, can be filled in soft gelatin capsules and then will generate a drug containing micro-emulsion with a large surface area upon dispersion in the gastrointestinal tract. The emulsions will further facilitate the absorption of the drug due via intestinal lymphatic pathway and by partitioning of drug into the aqueous phase of intestinal fluids. In the present review, an overview of SMEDDS as a key technology for formulating lipophilic drugs and various factors that potentially affect the oral bioavailability of such drugs are presented.

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Bioavailability of seocalcitol

Cited by 101 publications

References 28 publications

Lipid-based systems as a promising approach for enhancing the bioavailability of poorly water-soluble drugs

Lipid-based systems as a promising approach for enhancing the bioavailability of poorly water-soluble drugs

Liquid and Solid Self-Emulsifying Drug Delivery Systems (SEDDs) as Carriers for the Oral Delivery of Azithromycin: Optimization, In Vitro Characterization and Stability Assessment

Self-Micro Emulsifying Drug Delivery Systems (Smedds): A Review on Physico-Chemical and Biopharmaceutical Aspects

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