Current Issue : January - March Volume : 2019 Issue Number : 1 Articles : 5 Articles
This study aims at developing and evaluating reconstitutable dry suspension (RDS)\nimproved for dissolution rate, oral absorption, and convenience of use of poorly water-soluble\ncelecoxib (CXB). Micro-sized CXB particle was used to manufacture nanosuspension by using bead\nmilling and then RDS was made by spray-drying the nanosuspension with effective resuspension\nagent, dextrin. The redispersibility, morphology, particle size, crystallinity, stability, dissolution,\nand pharmacokinetic profile of the RDS were evaluated. RDS was effectively reconstituted into\nnanoparticles in 775.8 ± 11.6 nm. It was confirmed that CXB particles are reduced into needle-shape\nones in size after the bead-milling process, and the description of CXB was the same in the\nreconstituted suspension. Through the CXB crystallinity study using differential scanning calorimetry\n(DSC) and XRD analysis, it was identified that CXB has the CXB active pharmaceutical ingredient\n(API)â??s original crystallinity after the bead milling and spray-drying process. In vitro dissolution\nof RDS was higher than that of CXB powder (93% versus 28% dissolution at 30 min). Furthermore,\nRDS formulation resulted in 5.7 and 6.3-fold higher area under the curve .... and peak\nconcentration (Cmax) of CXB compared to after oral administration of CXB powder in rats. Collectively,\nour results suggest that the RDS may be a potential oral dosage formulation for CXB to improve its\nbioavailability and patient compliance....
This study aimed to evaluate and compare, using the methodology of Franz diffusion cells,\nthe ketoprofen (KTP) releasing profiles of two formulations: A gel and a conventional suspension.\nThe second aim was to show that this methodology might be easily applied for the development\nof semi-solid prototypes and claim proof in pre-formulation stages. Drug release analysis was\ncarried out under physiological conditions (pH: 5.6 to 7.4; ionic strength 0.15 M; at .... for\n24 h. Three independent vertical Franz cells were used with a nominal volume of the acceptor\ncompartment of 125 mL and a diffusion area of 2.5 cm2. Additionally, two different membranes\nwere evaluated: A generic type (regenerated cellulose) and a transdermal simulation type (Strat-M®).\nThe KTP permeation profiles demonstrated that depending on the membrane type and the vehicle\nused, the permeation is strongly affected. High permeation efficiencies were obtained for the\ngel formulation, and the opposite effect was observed for the suspension formulation. Moreover,\nthe permeation studies using Strat-M membranes represent a reproducible methodology, which is\neasy to implement for pre-formulation stage or performance evaluation of semi-solid pharmaceutical\nproducts for topical or transdermal administration....
Background: The use of resveratrol as a dietary supplement is limited because it is easily\noxidized and, after oral ingestion, it is metabolized into enterocytes and hepatocytes. Thus, new\nformulations are needed in order to improve its oral bioavailability. Objective: The objective of\nthis study was to develop and characterize a gastro-resistant formulation of resveratrol for oral\nadministration as a dietary supplement. Method: Resveratrol was encapsulated in Eudragit-coated\npectin-alginate microparticles. Results: The microparticle size was about 1450 .., with an\nencapsulation efficiency of 41.72% ± 1.92%. The dissolution assay conducted, as specified in the\nEuropean Pharmacopoeia for delayed-release dosage forms, revealed that our microparticles were\ngastro-resistant, because the resveratrol percentage released from microparticles in acid medium was\nless than 10%. In addition, the high-performance liquid chromatographic (HPLC) method developed\nfor resveratrol content quantification in the microparticles was validated according to International\nCouncil for Harmonisation (ICH) Q2 (R1) guidelines. Finally, the biological activity of resveratrol was\ninvestigated in 3T3-L1 mature adipocytes, concluding that the encapsulation process does not affect\nthe activity of resveratrol. Conclusion: In summary, the gastro-resistant microparticles developed\ncould represent a suitable method of including resveratrol in dietary supplements and in functional\nfoods used in obesity therapy....
Raloxifene (RXF) is a hormone-like medication used for treating postmenopausal\nosteoporosis and estrogen-dependent breast cancer, yet associated with bad low bioavailability\ndue to poor solubility. This study was intended to develop cyclodextrin/chitosan nanoparticles\n(ccNPs) for oral delivery of RXF in order to enhance the oral bioavailability. RXF-loaded ccNPs\n(RXF-ccNPs) were prepared by cyclodextrin inclusion followed by complexation with chitosan.\nRXF-ccNPs were fully characterized by particle size, morphology and in vitro drug release. The oral\ndelivery efficacy and transepithelial transport potential were evaluated by pharmacokinetics, in\nsitu single-pass intestinal perfusion, cellular uptake and ex vivo imaging. The resulting RXF-ccNPs\nwere around 165 nm in particle size with a narrow distribution. The oral bioavailability of RXF\nwas enhanced by 2.6 folds through ccNPs compared to RXF suspensions in rats. It was shown that\nRXF-ccNPs could improve the intestinal permeability of RXF, increase the cellular uptake of RXF and\nfacilitate its transport across the absorptive epithelia. The results indicate that our developed ccNPs\nbased on sulfobutylether ... cyclodextrin and oligochitosan are a promising vehicle to orally deliver\npoorly water-soluble drugs over and above RXF....
Treatment for herpes simplex virus-1 and -2 (HSV-1 and -2) patients who suffer from recurrent outbreaks consists of multiple daily\ndoses of the antiviral drugs acyclovir (ACV), penciclovir, or their more orally bioavailable derivatives valacyclovir or famciclovir.\nDrug troughs caused by missed doses may result in viral replication, which can generate drug-resistant mutants along with\nclinical sequelae. We developed a molecularly homogeneous mixture of ACV with the bioerodable polymer polycaprolactone.\nThrough scanning electronmicroscopy, infrared spectroscopy, gel permeation chromatography, 1HNMR, and differential scanning\ncalorimetry, ourmethod of combining drug and polymer, termedVolatile Acid-Solvent Evaporation (VASE), does not compromise\nthe integrity of polymer or drug. Furthermore, VASE creates materials that deliver therapeutic amounts of drug consistently for\napproximately two months. Devices with high enough drug loads diminish primary infection of HSV-1 in Vero cells to the same\nlevel as seen with a single dose of ACV. Our data will lead to further experiments in animal models, demonstrating efficacy in\npreventing reactivation of these viruses with a single intervention, and with other antiviral drugs amenable to such manipulation.\nAdditionally, this type of treatment would leave no trace after its useful lifetime, as drug is released and polymer matrix is degraded\nin vivo....
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