Development of orally disintegrating tablets comprising controlled-release multiparticulate beads.

Melperone is an atypical antipsychotic agent that has shown a wide spectrum of neuroleptic properties, particularly effective in the treatment of senile dementia and Parkinson's-associated psychosis, and is marketed in Europe as an immediate-release (IR) tablet and syrup. An orally disintegrating tablet (ODT) dosage form would be advantageous for patients who experience difficulty in swallowing large tablets or capsules or those who experience dysphagia. Controlled-release (CR) capsule and ODT formulations containing melperone HCl were developed with target in vitro release profiles suitable for a once-daily dosing regimen.

A folate receptor-targeted lipid nanoparticle formulation for a lipophilic paclitaxel prodrug.

Purpose: The anticancer drug paclitaxel has poor aqueous solubility and is difficult to formulate in a lipid-based formulation due to its limited lipid solubility. Paclitaxel-7-carbonyl-cholesterol (Tax-Chol), a prodrug of paclitaxel with increased lipophilicity, was therefore synthesized and evaluated for incorporation into a lipid nanoparticle (LN) formulation, which also contained folate-polyethylene glycolcholesterol (f-PEG-Chol) as a ligand that targets the tumor marker folate receptor (FR). This novel formulation was designed for prolonged systemic circulation and selective targeting of tumor cells with amplified FR expression.

Optical characteristics of the canine prostate at 665 nm sensitized with tin etiopurpurin dichloride: need for real-time monitoring of photodynamic therapy.

Purpose: Photodynamic therapy (PDT) is an emerging, minimally invasive therapy for prostate cancer that depends on the sequestration of a photosensitizing drug within targeted tissue. The photosensitizer is subsequently activated by light of a specific wavelength, resulting in destruction of the targeted tissue. Successful treatment requires knowledge of the optical properties of the target tissue, a critical element for therapy.

Synthesis and evaluation of a hematoporphyrin derivative in a folate receptor-targeted solid-lipid nanoparticle formulation.

Purpose: This study was aimed at the synthesis, formulation and in vitro evaluation of folate receptor (FR)-targeted solid-lipid nanoparticles (SLNs) as a carrier for a lipophilic derivative of the photosensitizer hematoporphyrin (Hp), in FR-overexpressing tumor cells.

Materials And Methods: FR-targeted hematoporphyrin-stearylamine (HpSa) SLN composed of Triolein:Egg-phosphatidylcholine (EPC):Tween-80 (T-80) (64:25:10), with 0.5 mole % of folate-polyethyleneglycol-cholesterol (FPC) or polyethyleneglycol-distearoylphosphatidylethanolamine (PEG-DSPE), were prepared by ethanol injection method.

A folate receptor-targeted emulsion formulation for paclitaxel.

Purpose: This study was aimed at the formulation and an in vitro evaluation of folate receptor (FR)-targeted emulsions as carriers for the lipophilic drug paclitaxel, in FR-overexpressing tumor cells.

Materials And Methods: FR-targeted paclitaxel emulsions (< 100 nm) composed of Tween-80:triolein:cholesterol:oleic acid:egg-phosphatidylcholine (EPC) (10:30:19.5:30:10), with 0.

Folate receptor-targeted liposomes as possible delivery vehicles for boron neutron capture therapy.

Background: The folate receptor is amplified in a variety of human tumors including over 90% of ovarian carcinoma. FR-targeted liposomes have previously been used by us to selectively deliver entrapped boron-containing compounds to tumor cells for neutron capture therapy (NCT). In the present study we have evaluated the delivery of Na3(B20H17NH3), which has been loaded into FR-targeted liposomes, in mice bearing xenograft implants of FR (+) KB subcutaneous tumor.

Formulation kit for liposomal doxorubicin composed of lyophilized liposomes.

Background: Doxorubicin can be loaded into preformed liposome by remote loading. Lyophilization of liposomes results in particle size increase and content leakage. Cryoprotectants have been used to improve the stability of liposomal formulations during lyophilization.