Preparation and Immunological Evaluation of Organic Acid Salts of Levamisole

Abstract

Levamisole (LMS), the levo-isomer of tetramisole, is an anthelminthic belonging to a class of synthetic imidazothiazole derivatives, as well as an immunomodulator which can enhance the immune responses [1][2][3][4][5] . Due to the poor solubility and instability in water, its hydrochloride (levamisole hydrochloride, LH) is commonly used in clinical. However, LH still has problems of low bioavailability and side effects, such as a certain stimulus to the human body. In the past decade, a large number of researches have been increasingly reported with respect to chemical modifications of drugs, such as esterification 6 , acylation 7 , amidation 8 , alkylation 9 , anhydride formation 10 , salt formation [11][12][13][14][15][16][17] , ring opening and formation 18,19 . As reported, chemical modifications have many advantages such as improving the solubility, stability and bioavailability of drugs, reducing toxic reactions, enhancing pharmacological effects, extending drug action, making other drug dosage forms and delivery systems possible or more excellent, etc.Salt formation is a simple and effective chemical modification, which can influence a number of physicochemical properties of the parent drug, including solubility, dissolution rate, stability and hygroscopicity 11 . As a result, different salts of drugs may bring about different pharmacokinetic and pharmacodynamic qualities and therefore different clinical qualities; some even may show intrinsic toxicity 14 . Levamisole base has a tertiary nitrogen atom, whose lone pair of electrons can accept

Tunable construction of multi-shelled hollow carbonate nanospheres and their potential applications

“…The selection of the organic acid salts but not inorganic salts as the reactants is innovative and crucial because it could provide metal ions and carbonate ions simultaneously for MHCN formation. 9 The strategy avoids the tedious operation of having to add two or more reagents, and the difficulties in controlling the products and experimental conditions in the traditional synthesis of carbonate particles. 10 As shown in Scheme 1, CMSs (Carbonaceous Microspheres) and T-CMSs (CMSs treated with the ethanol solution of HCl) are used respectively as templates to adsorb the organic acid salts.…”