Evaluation of micelles incorporated into thermosensitive hydrogels for intratumoral delivery and controlled release of docetaxel: A dual approach for in situ treatment of tumors.

The in situ gelling hybrid hydrogel system has been reported to effectively concentrate chemotherapeutic drugs at the tumor site and sustain their release for a long period. DTX-micelles (docetaxel-loaded mixed micelles) are able to increase the solubility of DTX in water, and then a high drug loading rate of hydrogels can be achieved by encapsulating the docetaxel-loaded mixed micelles into the hydrogels. The thermosensitive nature of DTX-MM-hydrogels (thermosensitive hydrogels incorporated with docetaxel-loaded mixed micelles) can accelerate the formation of a depot of this drug-loaded system at the site of administration. Therefore, the hydrogels provide a much slower release compared with DTX-micelles and DTX-injection. An in vivo retention study has demonstrated that the DTX-MM-hydrogels can prolong the drug retention time and in vivo trials have shown that the DTX-MM-hydrogels have a higher antitumor efficacy and systemic safety. In conclusion, the DTX-MM-hydrogels prepared in this study have considerable potential as a drug delivery system, with higher tumor inhibition effects and are less toxic to normal tissues.

Preparation, characterization, and in vitro/vivo evaluation of polymer-assisting formulation of atorvastatin calcium based on solid dispersion technique.

Due to low solubility and bioavailability, atorvastatin calcium is confronted with challenge in conceiving appropriate formulation. Solid dispersion of atorvastatin calcium was prepared through the solvent evaporation method, with Poloxamer 188 as hydrophilic carriers. This formulation was then characterized by scanning electron microscopy, differential scanning calorimetry, powder X-ray diffraction and fourier transform infrared spectroscopy. Moreover, all these studies suggested the conversion of crystalline atorvastatin calcium. In addition, the drug solubility studies as well as dissolution rates compared with bulk drug and market tablets Lipitor were also examined. Furthermore, the study investigated the pharmacokinetics after oral administration of Lipitor and solid dispersion. And the AUC0-8   h and Cmax increased after taking ATC-P188 solid dispersion orally compared with that of Lipitor. All these could be demonstrated that ATC-P188 solid dispersions would be prospective means for enhancing higher oral bioavailability of ATC.

Evaluating bioequivalence of meloxicam tablets: is in-vitro dissolution test overdiscriminating?

OBJECTIVES: The aim of the study was to assess the impact of the differences in dissolution profiles of meloxicam tablets on the in-vivo bioavailability parameters after oral administration. METHODS: Compare in-vitro dissolution testing in the recommended media to evaluate in-vivo bioequivalence outcomes for the Biopharmaceutics Classification System Class II weak acidic drugs. Nine Beagle dogs received a single oral administration of each formulation (7.5 mg) in a three-way crossover design. KEY FINDINGS: The dissolution of meloxicam from both test products showed marked differences with that from the reference tablet in pH 1.0, 4.5 and 6.8 media at 50 or 75 rpm. Both formulations exhibiting slow or fast dissolution were then compared with the reference product for in-vivo bioequivalence study. Both products were bioequivalent with the reference tablet in either extent or rate of oral absorption. It indicated that the dissolution profiles which discriminated between the formulations in vitro did not accurately predict the in-vivo bioequivalence outcomes. CONCLUSIONS: Comparative dissolution profiles using similarity factor (f2 ) in the recommended media should be relaxed to fulfil the requirements for the development, scale-up and postapproval changes to immediate release oral solid dosage forms of meloxicam.

Glycyrrhizic acid: A promising carrier material for anticancer therapy.

Drug delivery systems have become an integral part of anticancer drugs today. Design of novel drug carriers may lead to significant enhancement in antineoplastic therapy. Glycyrrhizic acid (GL), which is the most important active ingredient extracted from the licorice root shows great potential as a carrier material in this field. Recent studies have indicated that the combination of GL and first-line drugs had better therapeutic effects on cancers. GL showed a series of anti-cancer-related pharmacological activities, such as broad-spectrum anti-cancer ability, resistance to the tissue toxicity caused by chemotherapy and radiation, drug absorption enhancing effects and anti-multidrug resistance (MDR) mechanisms, as a carrier material in drug delivery systems. This review introduced the current research progress on pharmacological mechanisms of GL and development of GL-based drug carriers in anti-cancer field to provide basis for the application prospects of GL. The design of novel GL-based drug delivery systems will bring new opportunities and challenges to anti-cancer therapy.