An injectable hybrid nanoparticle-in-oil-in-water submicron emulsion for improved delivery of poorly soluble drugs
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NANO EXPRESS
Open Access
An injectable hybrid nanoparticle-in-oil-in-water submicron emulsion for improved delivery of poorly soluble drugs Shuo Wang1, Hua Wang1, Wenquan Liang1* and Yongzhuo Huang2,3*
Abstract Poor drugability problems are commonly seen in a class of chemical entities with poor solubility in water and oil, and moreover, physicochemical instability of these compounds poses extra challenges in design of dosage forms. Such problems contribute a significant high failure rate in new drug development. A hybrid nanoparicle-in-oil-in-water (N/O/W) submicron emulsion was proposed for improved delivery of poorly soluble and unstable drugs (e.g., dihydroartemisinin (DHA)). DHA is known for its potent antimalarial effect and antitumor activity. However, its insolubility and instability impose big challenges for formulations, and so far, no injectable dosage forms are clinically available yet. Therefore, an injectable DHA N/O/W system was developed. Unlike other widely-explored systems (e.g., liposomes, micelles, and emulsions), in which low drug load and only short-term storage are often found, the hybrid submicron emulsion possesses three-fold higher drug-loading capacity than the conventional O/W emulsion. Of note, it can be manufactured into a freeze-drying form and can render its storage up to 6 months even in room temperature. The in vivo studies demonstrated that the PK profiles were significantly improved, and this injectable system was effective in suppressing tumor growth. The strategy provides a useful solution to effective delivery of such a class of drugs. Keywords: Poor solubility, Drug delivery, Nano emulsion, Nanoparticle, Dihydroartemisinin
Background Poor solubility of a chemical entity is a major obstacle affecting its drugability [1]. It is estimated that more than 40% of the new chemical entities generated in drug discovery programs are poorly soluble [2]. With growing interest in the role of modern pharmaceutics in early stage of drug discovery and development, rationale design of drug delivery systems for poorly soluble drugs has been widely explored, such as emulsions [3,4], solid lipid nanoparticles [5,6], micelles, and liposomes [7,8]. Emulsions are one of the most commonly used drug carriers for poorly water-soluble drugs due to the unique advantage in mass manufacturing, easy sterilization, and excellent physicochemical stability. However, there still remain two problems waiting to be solved, i.e., low drugloading capacity and quick drug release. Moreover, for * Correspondence: [email protected]; [email protected] 1 Zhejiang University College of Pharmaceutical Sciences, 388 Yuhangtang Road, Hangzhou 310058, China 2 Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 501 Hai-ke Road, Shanghai 201203, China Full list of author information is available at the end of the article
the drugs that remain insoluble in both water and oil, there is no satisfactory solution yet. As a case in point, dihydroartemisinin (DHA), a potent antimalarial drug [9,10], is poor
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