Formulation and characterization of albumin microspheres containing norcantharidate for liver tumor targeting

Abstract

The objectives of this study were first to encapsulate norcantharidate into albumin microspheres by the emulsion crosslinking method and second to characterize the microspheres in terms of the morphological examination, particle size, and encapsulation efficiency. The in vitro release of norcantharidate from the microspheres was studied by using the dialysis bag method. Pharmacokinetics and biodistribution studies were used to evaluate the advantages of microspheres than the conventional formulations. The microspheres prepared by crosslink emulsion were with uniform size, smooth surface, spherical shape, and disperse evenly. The particle size was uniform (13.3 ± 0.4 mm) and the encapsulation efficiency was 54.3 ± 4.18%. In vitro release indicated that the norcantharidate microspheres had a wellsustained release efficacy and fitted Korsmeyer's Peppas release model. In vivo studies showed that pharmacokinetics of norcantharidate microspheres could be described by the model of two-compartment after i.v. administration and had higher AUC inside liver and spleen than the injection group. No histological change occurred to the rat liver after the administration of norcantharidate microspheres.

Cantharidin inhibits competitively heme‐Fe(III) binding to the FA1 site of human serum albumin

“…Moreover, norcantharidin is effective against primary liver cancer . However, a drawback that limits the clinical use of cantharidin derivatives is their short half‐life, which would require frequent administrations to patients . To overcome this limitation, cantharidin derivatives have been incorporated into various microspheres that allow to prolong their half‐life and to minimize any risk of systemic toxicity …”

“…Recently, norcantharidin has been encapsulated into human serum albumin (HSA) microspheres since this plasma protein is a very appealing biocompatible carrier for drug delivery . Pharmacokinetic studies in rats showed that compared to the intravenous injection of free norcantharidin, the half‐life of the drug encapsulated into HSA microspheres increases.…”

“…Pharmacokinetic studies in rats showed that compared to the intravenous injection of free norcantharidin, the half‐life of the drug encapsulated into HSA microspheres increases. Therefore, HSA microspheres allow to rapidly distribute norcantharidin in the body, prolonging the drug circulation time and significantly increasing its bioavailability …”

“…Given the scientific interest for the anticancer properties of cantharidin derivatives and the advantages gained following their encapsulation into HSA microspheres, it appears very important to gain information concerning the binding mode of the lead compound cantharidin to HSA.…”

Budesonide-Loaded Guar Gum Microspheres for Colon Delivery: Preparation, Characterization and in Vitro/in Vivo Evaluation

“…Guar gum microspheres were prepared by the emulsion cross-linking technique [15,16]. Briefly, BUD (25 mg) and guar gum (125 mg) were added to 5 mL of methylene chloride.…”