Self-microemulsifying drug delivery system (SMEDDS) – challenges and road ahead

Dokania, Shambhu; Joshi, Amita

doi:10.3109/10717544.2014.896058

Cited by 247 publications

(201 citation statements)

References 152 publications

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“…Microemulsion (ME) formulations as well as self-emulsifying or self-micro/nano emulsifying drug delivery systems (SEDDS, SMEDDS and SNEDDS) have gained increased awareness as a valuable tactic to improve the oral bioavailability of lipophilic drugs (Gursoy & Benita, 2004;Araya et al, 2005a,b;Dokania & Joshi, 2014;Singh & Pai, 2014). The biopharmaceutical merits of ME and SEDDs include faster drug release by virtue of the small droplet sizes and large interfacial area promoting pancreatic lipase hydrolysis of lipids and fast drug dissolution with/ without bile salts-mixed micelles formation (Tarr & Yalkowsky, 1989).…”

Section: Emulsifiable Systemsmentioning

confidence: 99%

Strategies for oral delivery and mitochondrial targeting of CoQ10

Zaki

2014

Drug Delivery

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Coenzyme Q10 (CoQ10), also known as ubiquinone or ubidecarenone, is a powerful, endogenously produced, intracellularly existing lipophilic antioxidant. It combats reactive oxygen species (ROS) known to be responsible for a variety of human pathological conditions. Its target site is the inner mitochondrial membrane (IMM) of each cell. In case of deficiency and/or aging, CoQ10 oral supplementation is warranted. However, CoQ10 has low oral bioavailability due to its lipophilic nature, large molecular weight, regional differences in its gastrointestinal permeability and involvement of multitransporters. Intracellular delivery and mitochondrial target ability issues pose additional hurdles. To maximize CoQ10 delivery to its biopharmaceutical target, numerous approaches have been undertaken. The review summaries the current research on CoQ10 bioavailability and highlights the headways to obtain a satisfactory intracellular and targeted mitochondrial delivery. Unresolved questions and research gaps were identified to bring this promising natural product to the forefront of therapeutic agents for treatment of different pathologies.

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Section: Emulsifiable Systemsmentioning

confidence: 99%

Strategies for oral delivery and mitochondrial targeting of CoQ10

Zaki

2014

Drug Delivery

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“…15,16) Some well-known chemical compounds with low bioavailability were improved via SMEDDS. [17][18][19] The poor solubility and oral bioavailability of 20(S)-PPD challenge its clinical application. 20) In order to increase the solubility of 20(S)-PPD and improve the oral bioavailability, in this study, SMEDDS of 20(S)-PPD was prepared and evaluations were conducted including intestinal absorption, safe administration dosage and pharmacokinetics in vivo.…”

mentioning

confidence: 99%

Self-microemulsifying Drug Delivery System Improved Oral Bioavailability of 20(<i>S</i>)-Protopanaxadiol: From Preparation to Evaluation

Wang

et al. 2015

CHEMICAL & PHARMACEUTICAL BULLETIN

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20(S)-Protopanaxadiol (20(S)-PPD)is one type of sapogenin of protopanaxadiols and has a variety of pharmacological activities. In order to improve the dissolution of 20(S)-PPD as well as its oral bioavailability, a self-microemulsifying drug delivery system (SMEDDS) was utilized for 20(S)-PPD preparation. Following the preparation of the 20(S)-PPD SMEDDS, its dissolution, stability, and intestinal absorption in rats were studied, and the pharmacokinetics and optimal dosage after oral administration were evaluated. The dissolution tendency of the SMEDDS in phosphate buffered saline (PBS), 0.1 M HCl and distilled water was consistent. SMEDDS was stable under a condition of high temperature (40°C), high humidity or with strong light irradiation, or within 6 h in artificial digestive tracts. 20(S)-PPD SMEDDS was well-absorbed in all intestinal segments in rats. When the drug concentration was higher than 200 µg/mL or the perfusion flow was faster than 0.5 mL/min, passive diffusion of drug in the duodenum reached a saturated level. In addition, Pglycoprotein inhibitor did not affect the intestinal absorption of 20(S)-PPD SMEDDS. Pharmacokinetic study showed that T max in male rats was shortened significantly, while C max and area under the curve (AUC (0-t) ) were remarkably increased. The relative oral bioavailability of 20(S)-PPD SMEDDS was increased approximately three fold compared with the 20(S)-PPD carboxy methyl cellulose (CMC). 20(S)-PPD SMEDDS (100 mg/mL) was administered by gastric infusion to both mice and rats for 14 d. SMEDDS improved the oral bioavailability of 20(S)-PPD and reduced the necessary drug dosage. 20(S)-PPD SMEDDS could become a promising clinical alternative as an anti-tumor or antidepressant drug.Key words 20(S)-protopanaxadiol; self-microemulsifying drug delivery system; preparation; bioavailability; intestinal absorption; pharmacokinetics Panax ginseng is documented to tonify internal organs, benefit the spirit, suppress the fright as well as improve eyesight and intelligence.1) The long term application also facilitates relaxation and increases life span.2) Various chemical components were distinguished in Panax ginseng, including saponins, volatile oil, polysaccharides, amino acid and polypeptide, and microelements, of which ginsenosides are the main active ingredients, including oleanolic acid (OA), protopanaxadiol (PPD) and protopanaxatriol type (PPT).3) 20(S)-PPD ( Fig. 1) is one of aglycones of ginsenosides and has a wide range of pharmacological activities, especially in antitumor and neurological function recovery. [4][5][6][7][8] However, the low bioavailability of ginsenosides (1% for Rb 1 , 3.4% for Rb 2 , 1.9% for Rg 1 ) after oral administration restricts their clinical applications. 9-11)Importantly, PPD is the final active component after the absorption of ginsenosides in intestine. 12,13)

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“…), and the inclusion of polymers or other PIs within lipid-based formulations helps to maintain drug supersaturation after dispersion. Therefore, to reduce the amount of the surfactant and improve bioavailability, PIs are added to prepare the supersaturated self-emulsifying drug delivery systems (S-SEDDS) (76).…”

Section: (1) Formulation Aspectsmentioning

confidence: 99%

Bioavailability Improvement Strategies for Poorly Water-Soluble Drugs Based on the Supersaturation Mechanism: An Update

Yang¹,

Gong²,

Wang³

et al. 2016

J Pharm Pharm Sci

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-The formulation development for poorly soluble drugs still remains a challenge. Supersaturating drug delivery systems (SDDS) or drug delivery systems based on supersaturating provide a promising way to improve the oral bioavailability of poorly water-soluble drugs. In supersaturable formulations, drug concentration exceeds the equilibrium solubility when exposed to gastrointestinal fluids, and the supersaturation state is maintained long enough to be absorbed, resulting in compromised bioavailability. In this article, the mechanism of generating and maintaining supersaturation and the evaluation methods of supersaturation assays are discussed. Recent advances in different drug delivery systems based on supersaturating are the focus and are discussed in detail.

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Self-microemulsifying drug delivery system (SMEDDS) – challenges and road ahead

Cited by 247 publications

References 152 publications

Strategies for oral delivery and mitochondrial targeting of CoQ10

Strategies for oral delivery and mitochondrial targeting of CoQ10

Self-microemulsifying Drug Delivery System Improved Oral Bioavailability of 20(<i>S</i>)-Protopanaxadiol: From Preparation to Evaluation

Bioavailability Improvement Strategies for Poorly Water-Soluble Drugs Based on the Supersaturation Mechanism: An Update

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