Formulation of LDL Targeted Nanostructured Lipid Carriers Loaded with Paclitaxel: A Detailed Study of Preparation, Freeze Drying Condition, and In Vitro

In the present study, cholesterol nanostructured lipid carriers with various oleic acid content loaded with paclitaxel (PTX) were prepared by solvent emulsification-diffusion method using a Taguchi design. Size, zeta potential, entrapment efficiency, drug loading, and release percent of NLCs were measured. The results indicated that the most effective factors on the size were oleic acid content and surfactant percent. Zeta potential was more affected by the drug content. Drug to- lipid weight ratio was the most effective factor on entrapment efficiency and drug release from NLC. In the present work, the effect of lyophilization on the particle size and release properties of NLCs was also evaluated. The results revealed no differences between the characteristics of NLCs before and after freeze drying by using 25% w/w sorbitol as cryoprotectant. Cytotoxicity studies indicate that PTX associated with the NLC is also effective in HT-29 cell lines and enters the cancer cells selectively through the LDL receptor endocytic pathway. The IC50 values of free PTX solubilized in Cremophor EL and NLC-born PTX after 72 h exposure were  ng/mL and  ng/mL, respectively

Development and Evaluation of a Novel Pellet-Based Tablet System for Potential Colon Delivery of Budesonide

Budesonide, a potent glucocorticoid, is used for the treatment of inflammatory bowel diseases. Current available oral formulations of budesonide have low efficacy against ulcerative colitis because of the premature drug release in the upper part of the gastrointestinal tract. In this paper a pH- and time-controlled colon-targeted pellet-based tablet of budesonide was established. Pellet cores were prepared by extrusion-spheronization method and further coated with xanthan gum (barrier layer), Eudragit NE30D and L30D55 combination (inner layer), and Eudragit FS30 (as enteric layer) sequentially to achieve the required release profile. The coated pellets then compressed into tablets using inert tabletting granules of Cellactose or Pearlitol. Release studies, performed in simulated gastric, intestinal, and colon pH were used in sequence to mimic the gastrointestinal transit. The influence of formulation variables like barrier layer thickness, inner layer composition, and enteric coat thickness on drug release were investigated and the coated pellets that contained 12% weight gain in xanthan gum layer, Eudragit L30D55 and Eudragit NE30D with a ratio of 3 : 7 in inner layer with 30% weight gain and 25% weight gain in Eudragit FS layer were found to protect the drug release in stomach and small intestine and 83.35 ± 2.4 of budesonide was released at 24 h. The drug release from the tablets prepared using 40% Cellactose 80 as tableting excipient was found to be closely similar to that of uncompressed pellets

Effect of closed drainage system on edema and ecchymosis following rhinoplasty: a randomized clinical trial

Background: The aim of this study was to minimize edema and ecchymosis following rhinoplasty through a closed drainage system to address concealed hemorrhage.Methods: This study was designed as a prospective، double blinded, randomized contr-olled study. Fifty one patients who underwent septorhinoplasty were included in this study and divided in two groups. In group A, a closed drainage system was applied in the most dependent posterior septal area following septal harvesting. Concealed bloody secretions were drained out of mouth in a vacutaner tube during three concecutive post operative days. In control group, group B, exactly the same classic rhinoplasty opera-tion by the same surgeon was done as for study group except omitting the closed drainage system. Degree of supra-tip and eyelid edema was evaluated on post operative days through photographic and software image analysis. Edema and ecchymosis rating of eyelids and ecchymosis of paranasal and cheek area done based on photographic analysis by independent plastic surgeons using a defined grading system.Results: Eyelid ecchymosis was reduced significantly on post operative day 14 in the study group (P=0.03). Ecchymosis of paranasal and check was reduced considerably likewise on days 7 and 14 in group A using Mann-Whitney test (P=0.03). There was no significant deference regarding supra tip edema on post operative days. The same hold true for the eyelids edema.Conclusion: Significant decrement observed in eyelids ecchymosis on day 14 and para-nasal and cheek ecchymosis on postoperative days 7 and 14 in study group. There were no positive effects regarding supra tip and eyelid edema reduction using closed drainage system to evacuate concealed haemorrhage in posterior septum space. There could be different etio-pathologies for two common morbidities following rhinoplasty that should be addressed separately

Development and Evaluation of a Novel Pellet-Based Tablet System for Potential Colon Delivery of Budesonide

Budesonide, a potent glucocorticoid, is used for the treatment of inflammatory bowel diseases. Current available oral formulations of budesonide have low efficacy against ulcerative colitis because of the premature drug release in the upper part of the gastrointestinal tract. In this paper a pH-and time-controlled colon-targeted pellet-based tablet of budesonide was established. Pellet cores were prepared by extrusion-spheronization method and further coated with xanthan gum (barrier layer), Eudragit NE30D and L30D55 combination (inner layer), and Eudragit FS30 (as enteric layer) sequentially to achieve the required release profile. The coated pellets then compressed into tablets using inert tabletting granules of Cellactose or Pearlitol. Release studies, performed in simulated gastric, intestinal, and colon pH were used in sequence to mimic the gastrointestinal transit. The influence of formulation variables like barrier layer thickness, inner layer composition, and enteric coat thickness on drug release were investigated and the coated pellets that contained 12% weight gain in xanthan gum layer, Eudragit L30D55 and Eudragit NE30D with a ratio of 3 : 7 in inner layer with 30% weight gain and 25% weight gain in Eudragit FS layer were found to protect the drug release in stomach and small intestine and 83.35 ± 2.4 of budesonide was released at 24 h. The drug release from the tablets prepared using 40% Cellactose 80 as tableting excipient was found to be closely similar to that of uncompressed pellets

Effects of probiotic drop containing Lactobacillus rhamnosus, Bifidobacterium infantis, and Lactobacillus reuteri on salivary Streptococcus mutans and Lactobacillus levels

Aims: The aim of the present study was to evaluate the effect of a probiotic drop containing Lactobacillus rhamnosus, Bifidobacterium infantis, and Lactobacillus reuteri on salivary counts of Streptococcus mutans (SM) and Lactobacillus (LB) in children 3–6 years of age. Settings and Design: Sixty-one healthy children were randomly allocated into two parallel blocks in this double-blind, randomized controlled trial (IRCT2014120320202N1) from May to June 2015. Subjects and Methods: Finally 53 participants consumed five drops of placebo (n = 23) or probiotic (n = 30) every night for 2 weeks. Before intervention and 1 day after completion of the intervention, unstimulated salivary samples were collected, and microbiologic evaluations were carried out. Statistical Analysis: Data were analyzed with descriptive statistical methods Wilcoxon signed ranks, Mann–Whitney, and logistic regression. Results: SM level decreased significantly in probiotic group after intervention (P = 0.045), and there were significant differences in salivary SM counts after intervention between two groups (P = 0.04). In probiotic group, LB counts decreased significantly after intervention (P = 0.048); however, there were no significant differences between two groups (P = 0.216). Conclusions: Use of this probiotic drop decreased salivary counts of SM; however, LB counts did not change. In addition, use of the drop in children with higher salivary counts appeared to be more effective

Investigation of Properties of paper made from tensile wood and normal wood in Populus nigra

In this research Tension Wood (TW) and Normal Wood (NW) of Poplar were analyzed for pulp production using Kraft pulping process. After preparing samples, Biometric characteristics of the NW and TW fibers were measured and samples were converted to pulp. Pulp hand sheets mechanical and physical properties were measured and results were showed that NW fibers compared to TW fibers had a higher Rankle coefficient and aspect ratio. However the flexibility of NW fibers was better than TW fibers. Based on Results, although TW pulp yield was 13 percent greater than NW pulp yield but kappa number in TW was 45 percent lower than NW. Mechanical and physical properties of hand sheets indicated that the tensile and burst strengths of tension wood were comparatively lower than that of normal wood. Also the papers produced by equally mixture of TW fibers and NW fibers were showed higher tensile and burst strengths. Optical and color analyses of samples were showed an improvement in brightness and whiteness for TW hand sheets compared to NW papers. General speaking results were showed that presence of TW fibers inside pulp had not a significant effect on quality of produced pulp and papers

Ciljana isporuka budezonida u kolonu iz trostruko obloženih peleta: In vitro/in vivo evaluacija

Three layered pellets of budesonide were prepared for colon delivery by the extrusion-spheronization method. The coatings consisted of hydroxy propylmethyl cellulose (HPMC) (as barrier layer), Eudragit E (as rate controlling layer) and hydroxy propylmethyl cellulose acetate succinate (HPMC AS) (as enteric layer). The rate controlling layer was further modified using various pore formers. Dissolution studies were carried out at pHs of 1.2, 7.4 and 6.8. Pellet core composition and type and level of pore former affected the drug release from pellets. Pellets containing citric acid 20 % (m/m) in the cores coated with HPMC at a coating level of 6 % (m/m), Eudragit E containing Avicel RC 581 (30 %) as pore former at a coating level of 30 % (m/m) and HPMC AS at a coating level of 15 % (m/m) had the best release profiles. These pellets showed promising results in alleviating the conditions of an experimental model of colitis induced by trinitrobenzenesulfonic acid in rats.U radu je opisana priprava troslojnih peleta budezonida za ciljanu isporuku u kolonu metodom ekstruzije-sferonizacije. Obložni slojevi sastojali su se od hidroksipropilmetilceluloze (HPMC) (barijerni sloj), Eudragita E (kontrolni sloj) i hidroksipropilmetilceluloze acetat sukcinata (HPMC AS) (crijevni sloj). Sloj koji kontrolira oslobađanje je dalje modificiran koristeći različite tvari koje stvaraju pore. Oslobađanje je proučavano pri pH 1,2, 7,4 i 6,8. Sastav jezgre pelete, te vrsta i količina tvari koje stvaraju pore utjecale su na oslobađanje lijeka iz peleta. Pelete koje u jezgri sadrže 20 % (m/m) limunske kiseline obložene s HPMC (6 %, m/m), Eudragit E s Avicelom RC 581 kao tvari za stvaranje pora (30 %, m/m) i HPMC AS (15 %, m/m) imale su najbolji profil oslobađanja. Pelete su pokazale dobre rezultate u eksperimentalnom modelu kolitisa u štakora induciranog trinitrobenzensulfonskom kiselinom

Colon delivery of Budesonide Using Solid Dispersion in Dextran for the Treatment and Secondary Prevention of Ulcerative Colitis in Rat

Objectives: Ulcerative colitis is characterized by local inflamma-tion. Targeting drugs directly to the site of injury has the benefit of lower adverse effects and more effective therapy. The aim of this study was colon targeted delivery of budesonide to deliver the major part of the drug to the colon.Methods: Matrix tablets of budesonide from solid dispersion of drug with dextran were prepared using different drug to polymer ratios and three molecular weights of dextran. The physical evaluation and drug release behavior were studied. In vivo efficacy of the selected formulation against acetic acid induced colitis in rats was evaluated and compared to the control (untreated) and references (mesalasine and budesonide suspensions) groups.Results: The results showed that solid dispersion of budesonide with dextran in the ratio of 1:7 using molecular weight (MW) of 10,000 dextran (SDT710) released 25% of the drug in the first 6 hours and 100% in caecal and colonic contents. It could target the drug to colon with improvement in some of the inflammatory signs of induced ulcerative colitis in rat. Treatment with SDT710 could improve not only the percent of involvement also macroscopic damage parameters. The ma-croscopic parameters included weight/length ratio of the colon, ulcer area, damage score, and ulcer index reduced in comparison to the control group and conventional suspension of budesonide; however, only weight/length ratio was significant.Conclusions: In the experimental model studied, the new colonic delivery system significantly improved the efficacy of budesonide in the weight/length ratio of the colon in induced colitis in rats

Influence of carrier particle size, carrier ratio and addition of fine ternary particles on the dry powder inhalation performance of insulin-loaded PLGA microcapsules

The effects of carrier particle size, carrier ratio and addition of fine ternary agents on dry powder inhalation performance of insulin-loaded PLGA microcapsules were investigated. The use of mannitol with larger particle size in the lower carrier/microcapsules ratio led to higher deposition profiles of the drug. The fine spray dried mannitol and spray dried leucine as the ternary agents both decreased the deposition and dispersibility of microcapsules. It was concluded that addition of ternary component does not always improve aerosolization properties of DPI formulations. Carrier particle size, its flowability and carrier-drug ratio were shown to play an important role in DPI formulations. © 2010 Elsevier B.V