The Novel Formulation Design of Self-emulsifying Drug Delivery Systems (SEDDS) Type O/W Microemulsion I: Enhancing Effects on Oral Bioavailability of Poorly Water Soluble Compounds in Rats and Beagle Dogs

2005 ◽  
Vol 20 (4) ◽  
pp. 244-256 ◽  
Author(s):  
Hiroshi Araya ◽  
Shunsuke Nagao ◽  
Mikio Tomita ◽  
Masahiro Hayashi
Keyword(s):  
Drug Delivery ◽  
Oral Bioavailability ◽  
Drug Delivery Systems ◽  
Delivery Systems ◽  
Water Soluble ◽  
The Novel ◽  
Beagle Dogs ◽  
Formulation Design ◽  
Poorly Water Soluble

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

2013 ◽  
Vol 63 (4) ◽  
pp. 427-445 ◽  
Author(s):  
Katja Čerpnjak ◽  
Alenka Zvonar ◽  
Mirjana Gašperlin ◽  
Franc Vrečer
Keyword(s):  
Drug Delivery ◽  
Oral Bioavailability ◽  
Drug Delivery Systems ◽  
Water Solubility ◽  
Pharmaceutical Products ◽  
Delivery Systems ◽  
Water Soluble ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble

Abstract 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.

scholarly journals DESIGN AND DEVELOPMENT OF SELF-MICROEMULSIFYING DRUG DELIVERY SYSTEMS (SMEDDS) OF TELMISARTAN FOR ENHANCEMENT OF IN VITRO DISSOLUTION AND ORAL BIOAVAILABILITY IN RABBIT

2018 ◽  
Vol 10 (4) ◽  
pp. 117 ◽  
Author(s):  
Suvendu Kumar Sahoo ◽  
Padilam Suresh ◽  
Usharani Acharya
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Zeta Potential ◽  
Droplet Size ◽  
Oral Bioavailability ◽  
Drug Delivery Systems ◽  
Delivery Systems ◽  
Water Soluble ◽  
Poorly Water Soluble

Objective: The main purpose of this investigation was to prepare self-microemulsifying drug delivery system (SMEDDS) for enhancement of oral bioavailability of a poorly water soluble drug telmisartan (TLS), a BCS class II drug by improving its dissolution rate. Methods: Self-Emulsifying Drug Delivery Systems (SEDDS) of TLS were formulated using cinnamon essential oil as the oil phase, Gelucire 44/14 as the surfactant and Transcutol HP as co-surfactant. Drug-excipient interactions were studied by FTIR spectroscopy. The formulations were evaluated for its self-emulsifying ability, clarity, and stability of the aqueous dispersion after 48 h and the phase diagram was constructed to optimize the system. Selected formulations were characterized in terms of droplet size distribution, zeta potential, cloud point and were subjected to in vitro drug release studies. The bioavailability of optimized formulation was assessed in New Zealand white rabbits.Results: By considering smaller droplet size, higher zeta potential and faster rate of drug release the formulation TF9 was chosen as optimized SMEDDS formulations. TF9 was robust to different pH media and dilution volumes, remained stable after three cooling-heating cycles and after stored at 4 °C and 25 °C for 3 mo without showing a significant change in droplet size. The pharmacokinetic study in rabbits showed SMEDDS have significantly increased the Cmax and area under the curve (AUC) of TLS compared to suspension (P<0.05).Conclusion: SMEDDS can be an effective oral dosage form for enhancing aqueous solubility and improving oral bioavailability of poorly water soluble drugs.

Design and Characterization of Self-Nanoemulsifying Drug Delivery Systems of Rosuvastatin

2018 ◽  
Vol 11 (2) ◽  
pp. 4042-4052
Author(s):  
Bhikshapathi D. V. R. N. ◽  
Priya Keerthi
Keyword(s):  
Drug Delivery ◽  
Zeta Potential ◽  
Oral Bioavailability ◽  
Drug Delivery Systems ◽  
Ternary Phase Diagram ◽  
Delivery Systems ◽  
Water Soluble ◽  
Lipid Lowering ◽  
Tween 20 ◽  
Onset Of Action

Development of self-emulsifying drug delivery systems (SEDDS) are becoming more popular to improve the oral bioavailability of poorly water-soluble drugs. Rosuvastatin is a lipid-lowering agent used in patients suffering from dyslipidemia. It is a competitive inhibitor of 3-hydroxy 3-methyl glutaryl coenzyme A, which converts mevalonate to cholesterol. Rosuvastatin is a BCS class II (poor solubility) drug; hence, SNEDDS are being formulated to enhance oral bioavailability of the drug. In the present study, rosuvastatin SNEDDS were formulated using different oils, surfactant and co-surfactant. The optimized formulation F9 has composition of Las (PEG-8-Caprylic glycerides), Maisine 35-1 and Tween 20 as oil phase, surfactant and co-surfactant respectively. Composition of SNEDDS was optimized using Pseudo-ternary phase diagram, where the formulations showed increased self-emulsification with increased concentration of surfactants. Formulation F9 was found to be best formulation based on evaluation parameters. The particle size of the optimized SNEDDS formulation was found to be 10.9 nm & Z-Average of 55.6 nm indicating all the particles were in the nanometer range. The zeta potential of the optimized SNEDDS formulation was found to be -11.2 mV, which comply with the requirement of the zeta potential for stability. The developed rosuvastatin SNEDDS have the potential to minimize the variability in absorption and provide rapid onset of action of the drug.   

Sign in / Sign up

Export Citation Format

Share Document