Biomimetic aminoated mesoporous silica xerogel exhibiting chiral surface topology for delivery insoluble drug with multiple-controlled manners and improved oral adsorption
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Driven by the clinical demand on improving the oral bioavailability and reducing the side effects of insoluble drug, aminoated mesoporous silica xerogel (named L/d-BPEIN-MSX) with chiral surface topology was constructed through a facile, economical, and biomimetic strategy within 2 min, and served as the carrier of indomethacin (IMC). In the synthetic process, L/d-tartaric acid (L/d-TA) self-assembled with branched polyethyleneimine (BPEI) to endow chirality and synergistic promoted silica deposition, while 3-aminopropyl triethoxysilane (APTES) polycondensated with the silica source to form aminoated mesostructure. By premixed strategy, IMC can be in situ loaded into L/d-BPEIN-MSX with high efficiency, which then became active in circular dichroism (CD) spectra owing to induced chirality. Noteworthy, IMC-L/d-BPEIN-MSX significantly improved the release rate of IMC with multiple controlled release manners. That is, d-BPEIN-MSX had favorable drug release behavior which could respond to the chiral stimuli, whereas l-BPEIN-MSX exhibited advantageous chiral surface topology that was beneficial for bio-processes related to oral adsorption. Undoubtedly, they increased the bioavailability of IMC to 8–9 times, displayed good anti-inflammatory effect, and reduced the gastrointestinal irritation of IMC. In addition, L/d-BPEIN-MSX had low toxicity and irritation, and was proven to be biodegradable and biocompatible, which could meet the requirement for biomedical applications.Keywords:
Chirality
Triethoxysilane
Abstract The dispersibility of silane‐functionalized alumina nanoparticles (NPs) in syndiotactic polypropylene (sPP) was investigated. The Al 2 O 3 NP surface was modified with two different silane coupling agents, (3‐chloropropyl)triethoxysilane and (octyl)triethoxysilane, to create hydrocarbon groups, or their halogen derivatives, for the enhanced hydrophobic interaction with the sPP matrix. Transmission electron microscopy studies showed that the presence of hydrophobic groups improved the dispersibility of alumina NPs in the sPP matrix. A good dispersibility was found in both (3‐chloropropyl)triethoxysilane‐modified Al 2 O 3 /sPP nanocomposites and (octyl)triethoxysilane‐modified Al 2 O 3 /sPP nanocomposites. Copyright © 2010 John Wiley & Sons, Ltd.
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Polypropylene
Tacticity
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The absolute bioavailability of 8-methoxypsoralen in gelatin capsules and as a solution was studied in dogs. A dose of 2 mg kg-1 was given. Both for the solution and the gelatin capsules, a large variation in bioavailability was found between the different dogs. For the gelatin capsules in 1 dog out of 4 an absolute bioavailability of more than 100 per cent was found; for the solution a bioavailability of more than 100 per cent was found in all 4 dogs. Resorption was more rapid and bioavailability higher for the solution than for the gelatin capsules. Relative bioavailability of an emulsion and of a solution of 8-methoxypsoralen was studied in 2 dogs. A faster resorption and a higher bioavailability were found for the solution.
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In order to improve the surface properties of SiO 2 particles, SiO 2 particles were modified by vinyl triethoxysilane, SiO 2 particles and vinyl triethoxysilane modified SiO 2 particles were characterized by FTIR, SEM and XRD techniques. The results showed that vinyl triethoxysilane has been successfully grafted onto SiO 2 particles and basically there are no changes in the size of SiO 2 particles before and after the modification by vinyl triethoxysilane. XRD results show that the synthesized SiO 2 particles have certain crystallinity.
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This chapter contains sections titled: Introduction Oral Bioavailability Definition Cassette Dosing Across-species Prediction of Bioavailability In silico Models for Estimating Human Oral Bioavailability Quantitative Structure–Activity Relationship (QSAR) Approaches Molecular Properties Influencing Bioavailability Estimation of Bioavailability from Calculated Absorption ACE Inhibitors β-Blockers Calcium Antagonists In vitro Model for Predicting Oral Bioavailability in Human and other Species In vivo Method for Estimating Human Oral Bioavailability from Animal Pharmacokinetic Studies Factors to Consider in Optimizing Oral Bioavailability
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Several factors affecting the bioavailability of 5,5-diphenylhydantoin (I) and its sodium salt (I-Na) were examined in dogs in relation to meal and following results were obtained. The bioavailability of I was not appreciably affected by the volume of coadministered water in the range of 30-120 ml. The bioavailability of I was most excellent when I was administered 0.5 h after meal. Food intake 0.5 h after drug administration enhanced appreciably the bioavailability, but that 2 h after drug administration did hardly affect the bioavailability. The extent of bioavailability of I-Na was almost 100% of the dose in the range of 100-400 mg/dog when it was administered 0.5 h after meal. While, when I-Na was administered in the fasting state, the extent of bioavailability was about 60% of the dose. Food-induced enhancement of the bioavailability of I was independent of the food constituents. The bioavailability of I was increased about 1.5-fold and 2-fold with 10-fold increase in the specific surface area of I, in the nonfasting and the fasting states, respectively. In the experiments using the dogs with the chronically implanted fistula in the common bile duct, it was found that the bile was not a major factor contributing to the food-induced enhancement of the bioavailability of I. There was a good correlation between the bioavailability of I in dog and that in man.
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The bioavailability in beagle dogs and the dissolution rates of cyclandelate from five capsule preparations commercially available in Japan were measured. One of the capsules that showed an extremely low bioavailability in humans also showed the lowest bioavailability in beagle dogs, although the difference in bioavailability with the highest preparation was smaller than in humans. A significant correlation was obtained between the results of the studies in humans and beagles. However, the power of the test using beagles was extremely low in comparison with that in the human study. Food enhanced the bioavailability of cyclandelate from the capsules having the highest and lowest bioavailability in the fasted state in beagles as observed in the human study previously. The bioinequivalence of the cyclandelate capsules detected in the fasted state disappeared in the fed state in the beagle dog study, while the bioinequivalence still remained in the non-fasted state in human subjects. Thus bioequivalence testing in the fed state led to different results in both species. The most poorly bioavailable capsule in both species in the fasted state showed a slow dissolution rate by several dissolution methods with moderate stirring. In order to obtain a good correlation with in vivo bioavailability, a large volume of test solution and addition of Tween 80 were required. Extensive growth of whiskers (needle-like crystals) was observed in the entire capsule mass having the lowest bioavailability.
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In the present work, a simple method was used to develop composite curcumin-amine functionalized mesoporous silica nanoparticles (MSN). The nanoparticles were used to improve the bioavailability of curcumin in mice through oral administration. We investigated the effect of particle size on the release profile, solubility and oral bioavailability of curcumin in mice, including amine functionalized mesoporous silica micron-sized-particles (MSM) and MSN (100-200 nm). Curcumin loaded within amine functionalized MSN (MSN-A-Cur) had a better release profile and a higher solubility compared to amine MSM (MSM-A-Cur). The bioavailability of MSN-A-Cur and MSM-A-Cur was considerably higher than that of 'free curcumin'. These results indicate promising features of amine functionalized MSN as a carrier to deliver low solubility drugs with improved bioavailability via the oral route.
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