Effect of particle size and diluent type on critical parameters for disintegration of tablets containing croscarmellose sodium as a disintegrant

Purpose: The aim of the present work was to determine the effect of particle size and type of diluents on critical concentration for the disintegration of tablet formulations containing a physical binary mixture of a superdisintegrant (croscarmellose sodium, CS) and a diluent.Methods: The diluents used in this study were microcrystalline cellulose (MCC), dibasic calcium phosphate (DCP) and pregelatinized starch (PGS). Each diluent was divided into 2 different size ranges (small and large size)) and further mixed with 0 - 100 % CS. The binary mixture was compressed at controlled pressure, and the disintegration time and physical characteristic of the tablets were evaluated.Results: The point of CS concentration that markedly affected the disintegration time of the tablets was recorded as the critical concentration for disintegration. The results showed that the particle size of the diluent did not affect the disintegration time. The critical CS concentrations were 2 % for DCP and MCC tablets and 5 % for PGS tablet. Adding a small amount of CS improved the disintegration of the tablets. However, increasing the amount of CS in the formulation also affected the hardness of the tablets. The particle size of diluents had a significant effect on the critical concentration for tablet disintegration.Conclusion: Determining the type and appropriate amounts of diluent and disintegrant (percolating component) may be useful in the design of tablet formulations.Keywords: Disintegration, Percolation threshold, Croscarmellose sodium, Microcrystalline cellulose, Dibasic calcium phosphate, Pre-gelatinized starc

Mucoadhesive maleimide-functionalised liposomes for drug delivery to urinary bladder

Intravesical drug administration is used to deliver chemotherapeutic agents via a catheter to treat bladder cancer. The major limitation of this treatment is poor retention of the drug in the bladder due to periodic urine voiding. In this work, maleimide-functionalised PEGylated liposomes (PEG-Mal) were explored as mucoadhesive vehicles for drug delivery to the urinary bladder. The retention of these liposomes on freshly excised porcine bladder mucosa in vitro was compared with conventional liposomes, PEGylated liposomes, two controls (dextran and chitosan), and evaluated through Wash Out50 (WO50) values. PEG-Mal liposomes exhibited greater retention on mucosal surfaces compared to other liposomes. The penetration abilities of conventional, PEG-Mal-functionalised and PEGylated liposomal dispersions with encapsulated fluorescein sodium into the bladder mucosa ex vivo were assessed using a fluorescence microscopy technique. PEGylated liposomes were found to be more mucosa-penetrating compared to other liposomes. All liposomes were loaded with fluorescein sodium salt as a model drug and the in vitro release kinetics was evaluated. Longer drug release was observed from PEG-Mal liposomes

Pluronic lecithin organogel with d-limonene as a transdermal delivery system for Kaempferia parviflora extract

Kaempferia parviflora (KP) extract has been used in the Thai medicinal plant recipe, which the methoxyflavones are the main active compound. These compounds have low water solubility, high lipophilicity, and low bioavailability. The aim of this study was to develop the pluronic lecithin organogel (PLO) and PLO with d-limonene (PLO-L) for enhancing transdermal delivery of KP extract. These formulations were prepared and their physicochemical properties, stability, and in vitro skin permeation were evaluated. For the result, all formulations exhibited good physicochemical properties and stable under storage condition for 3 months. The permeation of KP extract-loaded PLO-L and PLO formulation showed significantly higher total methoxyflavones permeated through the skin than KP extract in water, which PLO-L provided the highest permeated flux of total methoxyflavones. This result suggested that d-limonene play a role as skin permeation enhancer. Organogel consisting of poloxamer 407 and lecithin also increased the skin permeation of KP extract. In conclusion, PLO-L could be a potential transdermal delivery system for KP extract

Pluronic lecithin organogel with d-limonene as a transdermal delivery system for

Kaempferia parviflora (KP) extract has been used in the Thai medicinal plant recipe, which the methoxyflavones are the main active compound. These compounds have low water solubility, high lipophilicity, and low bioavailability. The aim of this study was to develop the pluronic lecithin organogel (PLO) and PLO with d-limonene (PLO-L) for enhancing transdermal delivery of KP extract. These formulations were prepared and their physicochemical properties, stability, and in vitro skin permeation were evaluated. For the result, all formulations exhibited good physicochemical properties and stable under storage condition for 3 months. The permeation of KP extract-loaded PLO-L and PLO formulation showed significantly higher total methoxyflavones permeated through the skin than KP extract in water, which PLO-L provided the highest permeated flux of total methoxyflavones. This result suggested that d-limonene play a role as skin permeation enhancer. Organogel consisting of poloxamer 407 and lecithin also increased the skin permeation of KP extract. In conclusion, PLO-L could be a potential transdermal delivery system for KP extract

Influence of serum on DNA protection ability and transfection efficiency of cationic lipid-based nanoparticles for gene delivery

Cationic lipid-based nanoparticulate systems are delivery systems that has been widely used in pharmaceutical field including gene delivery. There are many barriers obstructing genetic materials and their delivery systems to reach the target. Serum is one of the imperative factor that should be investigated. Therefore, the aim of this study was to examine the effect of serum on DNA protection ability of spermine-liposomes and niosomes by evaluating the percentage of transfection efficiency in Hela cell and observing the DNA degradation band using agarose gel electrophoresis in the presence of serum. The results showed that the percentage of transfection efficiency of spermine-liposomes was dramatically decreased when serum is presented (p< 0.05). In contrast, whether or not the serum is presented, the spermine-niosomes showed no significant difference in transfection efficiency. Concisely, liposomes could slightly protect DNA from DNase in the serum, whereas, niosomes had potential ability to protect DNA from the enzymes in serum. This result revealed an advantage of the cationic niosomes system as a gene carrier over the cationic liposomes

Influence of serum on DNA protection ability and transfection efficiency of cationic lipid-based nanoparticles for gene delivery

Cationic lipid-based nanoparticulate systems are delivery systems that has been widely used in pharmaceutical field including gene delivery. There are many barriers obstructing genetic materials and their delivery systems to reach the target. Serum is one of the imperative factor that should be investigated. Therefore, the aim of this study was to examine the effect of serum on DNA protection ability of spermine-liposomes and niosomes by evaluating the percentage of transfection efficiency in Hela cell and observing the DNA degradation band using agarose gel electrophoresis in the presence of serum. The results showed that the percentage of transfection efficiency of spermine-liposomes was dramatically decreased when serum is presented (p< 0.05). In contrast, whether or not the serum is presented, the spermine-niosomes showed no significant difference in transfection efficiency. Concisely, liposomes could slightly protect DNA from DNase in the serum, whereas, niosomes had potential ability to protect DNA from the enzymes in serum. This result revealed an advantage of the cationic niosomes system as a gene carrier over the cationic liposomes