Application of diethylene glycol monoethyl ether in solubilization of poorly water-soluble drugs
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Journal of Pharmaceutical Investigation https://doi.org/10.1007/s40005-019-00454-y
REVIEW
Application of diethylene glycol monoethyl ether in solubilization of poorly water‑soluble drugs Eun‑Sol Ha1 · Seon‑Kwang Lee1 · Du Hyung Choi2 · Seong Hoon Jeong3 · Sung‑Joo Hwang4 · Min‑Soo Kim1 Received: 2 April 2019 / Accepted: 4 June 2019 © The Korean Society of Pharmaceutical Sciences and Technology 2019
Abstract Background Diethylene glycol monoethyl ether (DEGEE) is produced via the O-alkylation of ethanol with two ethylene oxide units, followed by distillation. It has a long history of safe use in food and personal-care products, and is used as an effective strong solubilizer in oral, topical, transdermal, and injectable human and veterinary pharmaceutical products. It has been used as a pharmaceutical solvent for many years under the trade name transcutol. DEGEE, a hydroalcoholic solvent, is gaining interest as a penetration/permeation enhancer, solubilizer, and surfactant for drug delivery systems. Area covered The physicochemical properties of DEGEE, the solubility data for drugs in DEGEE or DEGEE-water mixtures, and the applications of DEGEE in the solubilization of poorly water-soluble drugs are summarized in this review. Expert opinion DEGEE is a promising excipient as a solubilizer for many pharmaceutical products with enhanced drug absorption via oral, parenteral, and topical administration, as well as cosmetic products. Keywords Diethylene glycol monoethyl ether · Solubilizer · Solubility · Cosolvent · Transcutol
Introduction The development of new drug candidates and final dosage forms of drug products is a long and complex process. Aqueous solubility is one of the major challenges in the early stages of drug discovery, and techniques for enhancing the solubility are of great importance in the development of pharmaceutical dosage forms. Various formulations, such as amorphous solid dispersions, nanoemulsions, lipid-based formulations, inclusion complexes with cyclodextrins, and nanocrystals, have been developed to overcome the low aqueous solubility and bioavailability of various drugs (Hajjar et al. 2018; Liu et al. 2018; Williams et al. 2013a). * Min‑Soo Kim [email protected] 1
College of Pharmacy, Pusan National University, Busan 46241, Republic of Korea
2
Department of Pharmaceutical Engineering, Inje University, Gyeongnam 50834, Republic of Korea
3
College of Pharmacy, Dongguk University-Seoul, Gyeonggi 10326, Republic of Korea
4
College of Pharmacy and Yonsei Institute of Pharmaceutical Sciences, Yonsei University, Incheon 21983, Republic of Korea
In various drug carrier systems, excipients, which are an integral part of any formulation, can significantly impact the stability, processability, and performance of a dosage form (Sharma et al. 2017). In particular, the type of solubilizer employed has a significant impact on the design and development of the final product. Diethylene glycol monoethyl ether (DEGEE, Fig. 1) has a long history of use as a strong solubilizer in man
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