Surface Solid Dispersion of Ketoconazole on Trehalose Dihydrate using Spray Drying to Achieve Enhanced Dissolution Rate.

Ketoconazole (K) is a poorly water-soluble drug that faces significant challenges in achieving therapeutic efficacy. This study aimed to enhance the dissolution rate of ketoconazole by depositing spray-dried ketoconazole (SK) onto the surface of ground trehalose dihydrate (T) using spray drying. Ketoconazole-trehalose surface solid dispersions (SKTs) were prepared in ratios of 1:1 (SK1T1), 1:4 (SK1T4), and 1:10 (SK1T10), and characterized them using particle size analysis, scanning electron microscopy, powder X-ray diffraction, and in vitro dissolution studies.

Enhanced dissolution rates of glibenclamide through solid dispersions on microcrystalline cellulose and mannitol, combined with phosphatidylcholine.

Objective: This study aimed to investigate the impact of physical solid dispersions of spray-dried glibenclamide (SG) on the surface of microcrystalline cellulose (MC) and mannitol (M) surfaces, as well as their combination with phosphatidylcholine (P), on enhancing the dissolution rate of glibenclamide (G).

Methods: Solid dispersions were prepared using varying proportions of 1:1, 1:4, and 1:10 for SG on the surface of MC (SGA) and M (SGM), and then combined with P, in a proportion of 1:4:0.02 using spray drying.

N'-(3-Aminopropyl)-N-(3'-(carbamoyl cholesteryl) propyl)-glycine amide liposomes for delivery of pTRAIL-EGFP.

In this study, N'-(3-aminopropyl)-N-(3'-(carbamoyl cholesteryl) propyl)-glycine amide (A) and 1,2-dioleoyl-sn-glycero-3-phosphoethanolamine (DOPE, D) (AD) liposomes were synthesised at molar ratios of 50:25 (AD5025), 50:50 (AD5050) and 50:75 (AD5075) and complexed with plasmid, pTRAIL-EGFP. AD liposome/pTRAIL-EGFP were evaluated for their complex ability, particle size, polydispersity index, zeta potential, expression of pTRAIL-EGFP, cytotoxicity, cell growth inhibition and apoptosis induction in KB cells. AD liposomes complexed completely with pTRAIL-EGFP at AD liposome/DNA ratios of above 4.

Synergistic Inhibition of Human Carcinoma Cell Growth Co-Delivery of p53 Plasmid DNA and bcl-2 Antisense Oligodeoxyribonucleotide by Cholic Acid-modified Polyethylenimine.

Background/aim: This study investigated the co-delivery of plasmid DNA and antisense oligodeoxyribonucleotide (AS ODN) into carcinoma cells by cholic acid-modified polyethylenimine (PEI-CA).

Materials And Methods: PEI-CA/plasmid DNA and AS ODN complexes were formulated and evaluated for delivery of plasmid DNA and AS ODN in HeLa cells. The efficiency of co-delivery of plasmid DNA and AS ODN was evaluated by cell growth inhibition using p53 and bcl-2 AS ODN.

Co-delivery of plasmid DNA and antisense oligodeoxyribonucleotide into human carcinoma cells by cationic liposomes.

This study aimed to evaluate the co-delivery of cationic liposome/plasmid DNA complexes and cationic liposome/antisense oligodeoxyribonucleotide (AS ODN) complexes in HeLa human cervical carcinoma cells. Dimethyldioctadecyl ammonium bromide (DDAB): dioleoyl phosphatidylethanolamine (DOPE) liposome/plasmid DNA complexes, and DDAB:DOPE liposome/AS ODN complexes were formulated and characterized in terms of agarose gel electrophoretic mobility, particle size and zeta potential. The complexes were evaluated for delivery of pEGFP plasmid DNA and AS ODN in HeLa cells.

Growth inhibition and chemosensitization of human carcinoma cells by human serum albumin-coated liposomal antisense oligodeoxyribonucleotide against bcl-2.

Previous study has shown human serum albumin (HSA) coated liposomes can deliver bcl-2 antisense oligodeoxyribonucleotide (ODN) into KB carcinoma cells, and decrease bcl-2 mRNA and protein expression level. In the current study, cell growth inhibition and chemosensitization of KB cells were evaluated. Liposomes composed of dimethyldioctadecyl ammonium bromide/egg phosphatidylcholine/α-tocopheryl polyethylene glycol 1000 succinate (58:40:2 molar ratio) complexed with bcl-2 antisense ODN and coated with HSA were examined for cell growth inhibition and sensitization to a commonly used chemotherapeutic drug, doxorubicin.

Transferrin-conjugated lipid-coated PLGA nanoparticles for targeted delivery of aromatase inhibitor 7alpha-APTADD to breast cancer cells.

Transferrin (Tf)-conjugated lipid-coated poly(d,l-lactide-co-glycolide) (PLGA) nanoparticles carrying the aromatase inhibitor, 7alpha-(4'-amino)phenylthio-1,4-androstadiene-3,17-dione (7alpha-APTADD), were synthesized by a solvent injection method. Formulation parameters including PLGA-to-lipid, egg PC-to-TPGS, and drug-to-PLGA ratios and aqueous-to-organic phase ratio at the point of synthesis were optimized to obtain nanoparticles with desired sizes and drug loading efficiency. The optimal formulation had a drug loading efficiency of 36.

Disulfide-linked liposomes: effective delivery vehicle for Bcl-2 antisense oligodeoxyribonucleotide G3139.

Background: Disulfide-linked oligodeoxyribonucleotide (ODN) liposomes were formulated and evaluated for the delivery of antisense ODN G3139 in KB human oral carcinoma cells.

Materials And Methods: Liposomes composed of 1,2-di-(9Z-octadecenoyl)-3-trimethylammo-nium-propane (DOTAP)/egg phosphatidylcholine/alpha-tocopheryl polyethylene glycol 1000 succinate were incorporated with hydrophobized disulfide-linked ODN. Disulfide-linked ODN liposomes were characterized for their size, ODN intracellular delivery, Bcl-2 mRNA and protein expression, growth inhibition, and chemosensitization.

Efficient delivery of antisense oligodeoxyribonucleotide g3139 by human serum albumin-coated liposomes.

Human serum albumin (HSA)-coated liposomal formulations were synthesized and evaluated for the delivery of antisense oligodeoxyribonucleotide (ODN) G3139 in KB human oral carcinoma cells. Liposomes composed of dimethyldioctadecyl ammonium bromide/egg phosphatidylcholine/alpha-tocopheryl polyethylene glycol 1000 succinate (58:40:2 molar ratio) complexed with G3139 and coated with HSA were investigated for Bcl-2 downregulating activity. Cellular uptake of HSA-coated liposome-ODN complexes was more efficient than the uncoated liposome-ODN complexes.

Effect of depsipeptide on in vitro transfection efficiency of PEI/DNA complexes.

Unlabelled: The aim of this study was to investigate the effect of depsipeptide on the in vitro transfection efficiency of PEI/DNA complexes.

Materials And Methods: PEI (polyethylenimine 25K) formed a complex with pcDNA3-CMV-Luc and was investigated for its transfection efficiency in KB human oral carcinoma and Raji human lymphoma cell lines. The transfected cells were then incubated with different concentrations of depsipeptide for 24 h and examined for the transfection efficiency and cell viability.

Evaluation of chitosan salts as non-viral gene vectors in CHO-K1 cells.

The aim of this study was to investigate chitosan/DNA complexes formulated with various chitosan salts (CS) including chitosan hydrochloride (CHy), chitosan lactate (CLa), chitosan acetate (CAc), chitosan aspartate (CAs) and chitosan glutamate (CGl). They were assesed for their DNA complexing ability, transfection efficiency in CHO-K1 (Chinese hamster ovary) cells and their effect on cell viability. CHy, CLa, CAc, CAs and CGl, MW 45kDa formed a complex with pcDNA3-CMV-Luc at various N/P ratios.

In vitro gene transfer using cationic vectors, electroporation and their combination.

Background: The aim of this study was to investigate the transfection efficiency of cationic vectors (polyethylenimine; PEI25K and lipofectamine), electroporation and their combination in the human cancer cell lines, Raji human lymphoma and KB human oral carcinoma.

Materials And Methods: Raji human lymphoma and KB human oral carcinoma cell lines were transfected with pcDNA3-CMV-Luc at various N/P ratios of cationic vectors and voltages of electroporation, as well as with a combination of the cationic vectors and electroporation.

Results: The major findings were: (a) cationic vectors or electroporation alone increased transfection efficiency; (b) cationic vectors inhibited the transfection efficiency by electroporation.

Chitosan lactate as a nonviral gene delivery vector in COS-1 cells.

The purpose of this research was to evaluate chitosan lactate (CL) of different molecular weights (MWs) as a DNA complexing agent for its efficiency in transfecting COS-1 cells (green monkey fibroblasts) and its effect on cell viability compared with polyethylenimine (PEI), a commercially available cationic polymer. CL and chitosan base dissolved in dilute acetic acid (chitosan acetate [CA]) of different MWs (20, 45, 200, 460 kDa) and N/P ratios (2:1, 4:1, 8:1, 12:1, 24:1) formed complexes with pSV beta-galactosidase plasmid DNA. The complexes were characterized by agarose gel electrophoresis and investigated for their ability to transfect COS-1 cells compared with PEI.

Antioxidative and neuroprotective activities of extracts from the fruit hull of mangosteen (Garcinia mangostana Linn.).

Objective: The aim of this study was to investigate the antioxidative and neuroprotective activities of various extracts from the fruit hull of mangosteen (Garcinia mangostana Linn., GM).

Materials And Methods: Four extracts: water, 50% ethanol, 95% ethanol and ethyl acetate, were used.