PHYSICAL PROPERTIES OF PROLIPOSOME FOR INDUSTRIAL QUALITY CONTROL AND RECONSTITUTION OF PROLIPOSOME IN PORCINE INTESTINAL MUCOSA

Objective: The aim of this research was to examine the physical properties of proliposome granules for industrial quality control and to develop the proliposome tablet. The reconstitution of proliposome into liposome in porcine intestinal mucosa was also examined.Methods: Proliposome granules of bovine serum albumin (BSA) were prepared by granulation method with lecithin and cholesterol as coating lipid. The physical properties which were granular size, flow-ability, moisture content and adsorption isotherm of granules were examined and set as quality control (QC) standards. The obtained proliposome granules were further compressed into tablets with addition of filler/binders. Proliposome granules were also studied in porcine intestinal mucosa at specific time of 0, 5, 10 and 20 minutes to observe the reconstitution of proliposome into liposome.Results: Granular size was decreased regarding the drop of BSA while the amount of lipid had no obvious effect on granular size. Granular size with properties of fair flow-ability and the granular moisture of less than 1.5% was capable for the good tablet compression. These parameters could be set as the standard for quality control of proliposome granules. Proliposome granules displayed type V of BET adsorption isotherm which could be exploited as the fingerprint of proliposome formula and set as QC standard. The reconstitution of proliposome into liposome by mucus on surface of small intestine was clearly observed at 10 minutes onward. The addition of PVP as dry binder along with Avicel® increased the hardness of proliposome tablet, suitable for further experiment of an enteric coating.Conclusion: Industrial quality control of proliposome granules could be accessed by physical properties of granules. PVP combined with Avicel® were the appropriate binders for proliposome tablet compression. The reconstitution of proliposome into liposome could be displayed on the surface of the small intestine.Â

Development of Acyclovir-loaded Bovine Serum Albumin Nanoparticles for Ocular Drug Delivery

The aim of the present study was to develop acyclovir (ACV) ocular drug delivery systems of bovine serum albumin (BSA) nanoparticles as well as to assess their in vivo transcorneal permeability. The ACV-loaded nanoparticles with 4 % and 8 % drug loading were prepared by desolvation method. Morphology of the nanoparticles under scanning electron microscopy was spherical in shape and uniform in size. The mean sizes and entrapment efficiencies of ACV-loaded BSA nanoparticles were in the range of 125 - 132 nm and 15 - 25 %, respectively. Increasing the amount of ACV added into the formulation led to significant reduction of entrapment efficiency of nanoparticles. The results from in vivo transcorneal permeation studies revealed that ACV-loaded BSA nanoparticles could readily permeate through the rabbits’ cornea and bring about maximum ACV concentrations within 30 min and prolonged till 120 min

Development of Acyclovir-loaded Bovine Serum Albumin Nanoparticles for Ocular Drug Delivery

The aim of the present study was to develop acyclovir (ACV) ocular drug delivery systems of bovine serum albumin (BSA) nanoparticles as well as to assess their in vivo transcorneal permeability. The ACV-loaded nanoparticles with 4 % and 8 % drug loading were prepared by desolvation method. Morphology of the nanoparticles under scanning electron microscopy was spherical in shape and uniform in size. The mean sizes and entrapment efficiencies of ACV-loaded BSA nanoparticles were in the range of 125 - 132 nm and 15 - 25 %, respectively. Increasing the amount of ACV added into the formulation led to significant reduction of entrapment efficiency of nanoparticles. The results from in vivo transcorneal permeation studies revealed that ACV-loaded BSA nanoparticles could readily permeate through the rabbits’ cornea and bring about maximum ACV concentrations within 30 min and prolonged till 120 min

In Vitro

Mixed micelles of Pluronic F127 and D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) in different molar ratios (10 : 0, 7 : 3, 5 : 5, and 3 : 7) were prepared to characterize this system as nanocarriers for targeted delivery of chemotherapeutic agents. Their size, zeta potential, critical micelle concentration, drug loading content, entrapment efficiency, drug release, cytotoxicity, and stability in serum were evaluated in vitro by using doxorubicin as the model anticancer drug. The micellar sizes ranged from 25 to 35 nm. The 7 : 3 and 5 : 5 micellar combinations had lower critical micelle concentrations ( M) than the 10 : 0 combination ( M). The entrapment efficiencies of the 7 : 3, 5 : 5, and 3 : 7 micellar combinations were 72%, 88%, and 69%, respectively. Doxorubicin release was greater at acidic tumour pH than at normal physiological pH. The doxorubicin-loaded mixed micelles showed greater percent inhibition and apoptosis activity in human breast adenocarcinoma (MCF-7) and acute monocytic leukaemia (THP-1) cell lines than free doxorubicin did. The mixed micelles were also stable against aggregation and precipitation in serum. These findings suggest that Pluronic F127-TPGS mixed micelles could be used as nanocarriers for targeted anticancer-drug delivery

Preparation process by desolvation method for enhanced loading of acyclovir nanoparticles

The aim of this investigation was to qualitatively study on preparation process of enhanced loading acyclovir (ACV) in ACV-loaded bovine serum albumin (BSA) prepared by desolvation method with submerged jet of desolvating agent. The prepared ACV-loaded BSA nanoparticles in sterile water for injection (SWI) and isotonic trehalose solution were shown to be monodisperse with sizes of around 120 to 200 nm and zeta potentials of around -7 to -50 mV. However, those in phosphate buffer saline (PBS) were found to exhibit much larger sizes with polydispersity, which might be attributed to the effect of ionic strength. The loading efficiency was found to be around 60%. An increase in the amount of ACV added to the system could significantly improve the loading capacity by almost the same ratio, which may be due to molecular mixing behavior of submerged jet of desolvating agent

Development of Triamcinolone Acetonide-Loaded Nanostructured Lipid Carriers (NLCs) for Buccal Drug Delivery Using the Box-Behnken Design

The aim of this present work was to prepare triamcinolone acetonide (TA)-loaded nanostructured lipid carriers (TA-loaded NLCs) for buccal drug delivery systems using the Box-Behnken design. A hot homogenization method was used to prepare the TA-loaded NLCs. Spermaceti (X1), soybean oil (X2), and Tween 80 (X3) were used as solid lipid, liquid lipid, and stabilizer, respectively. The particle size of TA-loaded NLCs was lower than 200 nm and the zeta potential displayed the negative charge in all formulations. The percentage encapsulation efficiency (%EE) of the TA-loaded NLCs showed that it was higher than 80% for all formulations. Field emission scanning electron microscope (FESEM) confirmed that the size of TA-loaded NLCs was approximately 100 nm and energy-dispersive X-ray spectroscopy (EDS) confirmed that the TA could be incorporated in the NLC system. The Higuchi model gave the highest value of the R2, indicating that this model was a fit for the TA release profiles of TA-loaded NLCs. Confocal laser scanning microscopy (CLSM) was used to observe the drug penetration within the porcine buccal mucosa and Nile red-loaded NLCs showed significantly higher penetration depth at 8 h than at 2 h. Therefore, TA-loaded NLCs could be an efficient carrier for drug delivery through the buccal mucosa