Absorption Enhancement of Intrapulmonary Administered Insulin by Various Absorption Enhancers and Protease Inhibitors in Rats

1994 ◽  
Vol 46 (1) ◽  
pp. 14-18 ◽  
Author(s):  
Akira Yamamoto ◽  
Shinji Umemori ◽  
Shozo Muranishi
Keyword(s):  
Protease Inhibitors ◽  
Absorption Enhancement ◽  
Absorption Enhancers

scholarly journals Impact of Sodium N-[8-(2-Hydroxybenzoyl)amino]-caprylate on Intestinal Permeability for Notoginsenoside R1 and Salvianolic Acids in Caco-2 Cells Transport and Rat Pharmacokinetics

Molecules ◽  
2018 ◽  
Vol 23 (11) ◽  
pp. 2990 ◽  
Author(s):  
Ying Li ◽  
Dandan Yang ◽  
Chunyan Zhu
Keyword(s):  
Membrane Permeability ◽  
Cell Monolayer ◽  
Salvianolic Acid B ◽  
Absorption Enhancement ◽  
Enhancement Effect ◽  
Absorption Enhancers ◽  
Salvianolic Acid ◽  
Salvianolic Acids

For drugs with high hydrophilicity and poor membrane permeability, absorption enhancers can promote membrane permeability and improve oral bioavailability. Sodium N-[8-(2-hydroxybenzoyl)amino]caprylate (SNAC) is a new kind of absorption enhancer that has good safety. To investigate the absorption enhancement effect of SNAC on non-polar charged and polar charged drugs and establish the absorption enhancement mechanism of SNAC, SNAC was synthesized and characterized. Two representative hydrophilic drugs—notoginsenoside R1 (R1) and salvianolic acids (SAs)—were selected as model drugs. In vitro Caco-2 cells transport and in vivo rat pharmacokinetics studies were conducted to examine the permeation effect of SNAC on R1 and SAs. R1, rosmarinic acid (RA), salvianolic acid B (SA-B) and salvianolic acid B (SA-A) were determined to compare the permeation enhancement of different drugs. The MTT assay results showed that SNAC had no toxicity to Caco-2 cells. The transepithelial electrical resistance (TEER) of Caco-2 cell monolayer displayed that SNAC facilitated passive transport of polar charged SAs through the membrane of epithelial enterocytes. The pharmacokinetics results demonstrated that area under the curve (AUC) of RA, SA-B and SA-A with administration of SAs containing SNAC was 35.27, 8.72 and 9.23 times than administration of SAs. Tmax of RA, SA-B and SA-A were also prolonged. The AUC of R1 with administration of R1 containing SNAC was 2.24-times than administration of R1. SNAC is more effective in promoting absorption of SAs than R1. The study demonstrated that SNAC significantly improved bioavailability of R1 and SAs. What’s more, the effect of SNAC on absorption enhancement of charged drugs was larger than that of non-charged drugs. The current findings not only confirm the usefulness of SNAC for the improved delivery of R1 and SAs but also demonstrate the importance of biopharmaceutics characterization in the dosage form development of drugs.

scholarly journals Nasal Delivery of Recombinant Human Growth Hormone: In Vivo Evaluation with Pheroid™ Technology and N-Trimethyl Chitosan Chloride

2010 ◽  
Vol 13 (2) ◽  
pp. 263 ◽  
Author(s):  
Dewald Steyn ◽  
Lissinda Hester Du Plessis ◽  
Awie Kotze
Keyword(s):  
Growth Hormone ◽  
Human Growth Hormone ◽  
Recombinant Human Growth Hormone ◽  
Subcutaneous Administration ◽  
Human Growth ◽  
Absorption Enhancement ◽  
Control Group ◽  
Absorption Enhancers ◽  
Trimethyl Chitosan

Purpose. It was the aim of this study to investigate the possible enhancement of the absorption of recombinant human growth hormone (rhGH) in the nasal cavity, in the presence of a polymeric absorption enhancer, N-trimethyl chitosan chloride (TMC) and a fatty acid-based delivery system, Pheroid™. Methods. Two types of Pheroid™ formulations, Pheroid™ vesicles and Pheroid™ microsponges were characterized and evaluated with regard to particle size and morphology. In vivo bioavailability studies in rats were performed and the nasal bioavailability of Pheroid™ vesicles and Pheroid ™microsponges were compared relative to subcutaneous administration. The results were also compared with different N-trimethyl chitosan chloride (TMC) formulations, TMC H-L and TMC H-H, well studied absorption enhancers. Results. Pheroid™ vesicles and Pheroid™ microsponges showed a size distribution of approxiamately 2-3 µm and 3-4 µm for Pheroid™ vesicles and Pheroid™ microsponges respectively. Using specific RIA, the relative bioavailability of rhGH after comparison with subcutaneous injection was determined to be 38.9, 128.5, 39.9, 136.3, and 8.3 % for Pheroid™ microsponges, Pheroid™ vesicles, TMC H-H, TMC H-L and control group (intranasal rhGH alone), respectively. All the enhancers showed significant absorption enhancement (P < 0.05) with the highest effect observed with TMC H-L. Conclusion. All the enhancers may have promising potential as safe and effective nasal absorption enhancers of rhGH.

scholarly journals Absorption enhancement effect of piperine and chitosan on ganciclovir sol-id lipid nanoparticles: formulation, optimization and invivo pharmacoki-netics

2019 ◽  
Vol 10 (2) ◽  
pp. 1143-1151
Author(s):  
Ravindra Babu M ◽  
Ravi Prakash P ◽  
Devanna N
Keyword(s):  
Elimination Rate ◽  
Lipid Nanoparticles ◽  
Homogenization Method ◽  
Absorption Enhancement ◽  
Enhancement Effect ◽  
Pharmacokinetic Studies ◽  
Class Iii ◽  
Absorption Enhancers ◽  
Pure Drug

The purpose of the present study was to formulate Solid Lipid Nanoparticles (SLNs) of Ganciclovir (GCV) in combination with Chitosan and Piperine for absorption enhancement effect. GCV loaded SLNs were prepared by hot homogenization method, optimized and characterized. Formulated SLNs were incorporated with absorption enhancers and characterized for invitro absorption (with chicken intestine), histopathological and invivo pharmacokinetic studies. Invitro absorption studies revealed that the permeability coefficient of the prepared formulation is more when compared to the pure drug, so the permeability is more for prepared formulation. In vivo pharmacokinetic study showed a significant increase in the Cmax, AUC, biological half-life and decrease in elimination rate constant for prepared formulation compared to pure drug. Histopathological studies also showed mild reversible damage of epithelial cells with Chitosan which indicates the safety and efficacy of the formulation. Thus, GCV loaded SLNs prepared with Chitosan can be clinically promising for enhancing the oral, intestinal absorption of the said BCS Class-III drug.

scholarly journals Ceftriaxone Absorption Enhancement for Noninvasive Administration as an Alternative to Injectable Solutions

2018 ◽  
Vol 62 (12) ◽  
Author(s):  
Boubakar Ba ◽  
Karen Gaudin ◽  
Amélie Désiré ◽  
Thida Phoeung ◽  
Marie-Hélène Langlois ◽  
...  
Keyword(s):  
Neonatal Sepsis ◽  
Human Subjects ◽  
Rabbit Model ◽  
Absorption Enhancement ◽  
Rectal Absorption ◽  
Noninvasive Treatment ◽  
Absorption Enhancers ◽  
Treatment Delays ◽  
Resource Limited ◽  
Maximal Plasma

ABSTRACT Neonatal sepsis is a major cause of infant mortality in developing countries because of delayed injectable treatment, making it urgent to develop noninjectable formulations that can reduce treatment delays in resource-limited settings. Ceftriaxone, available only for injection, needs absorption enhancers to achieve adequate bioavailability via nonparenteral administration. This article presents all available data on the nonparenteral absorption of ceftriaxone in humans and animals, including unpublished work carried out by F. Hoffmann-La Roche (Roche) in the 1980s and new data from preclinical studies with rabbits, and discusses the importance of these data for the development of noninjectable formulations for noninvasive treatment. The combined results indicate that the rectal absorption of ceftriaxone is feasible and likely to lead to a bioavailable formulation that can reduce treatment delays in neonatal sepsis. A bile salt, chenodeoxycholate sodium salt (Na-CDC), used as an absorption enhancer at a 125-mg dose, together with a 500-mg dose of ceftriaxone provided 24% rectal absorption of ceftriaxone and a maximal plasma concentration of 21 µg/ml with good tolerance in human subjects. The rabbit model developed can also be used to screen for the bioavailability of other formulations before assessment in humans.

scholarly journals The Effect of Absorption-Enhancement and the Mechanism of the PAMAM Dendrimer on Poorly Absorbable Drugs

Molecules ◽  
2018 ◽  
Vol 23 (8) ◽  
pp. 2001 ◽  
Author(s):  
Juan Lu ◽  
Nannan Li ◽  
Yaochun Gao ◽  
Nan Li ◽  
Yifei Guo ◽  
...  
Keyword(s):  
Fluorescein Isothiocyanate ◽  
Pamam Dendrimer ◽  
Pamam Dendrimers ◽  
Absorption Enhancement ◽  
Dependent Manner ◽  
Pulmonary Absorption ◽  
Concentration Dependent Manner ◽  
Absorption Enhancers ◽  
Molecular Weights ◽  
Absorption Promoter

The polyamidoamine (PAMAM) dendrimer is a highly efficient absorption promoter. In the present study, we studied the absorption-enhancing effects and the mechanism of PAMAM dendrimers with generation 0 to generation 3 (G0–G3) and concentrations (0.1–1.0%) on the pulmonary absorption of macromolecules. The absorption-enhancing mechanisms were elucidated by microarray, western blotting analysis, and PCR. Fluorescein isothiocyanate-labeled dextrans (FDs) with various molecular weights were used as model drugs of poorly absorbable drugs. The absorption-enhancing effects of PAMAM dendrimers on the pulmonary absorption of FDs were in a generation- and concentration-dependent manner. The G3 PAMAM dendrimer with high effectiveness was considered to the best absorption enhancer for improving the pulmonary absorption of FDs. G3 PAMAM dendrimers at three different concentrations were non-toxic to Calu-3 cells. Based on the consideration between efficacy and cost, the 0.1% G3 PAMAM dendrimer was selected for subsequent studies. The results showed that treatment with a 0.1% G3 PAMAM dendrimer could increase the secretion of organic cation transporters (OCTs), OCT1, OCT2, and OCT3, which might be related to the absorption-enhancing mechanisms of the pulmonary absorption of FDs. These findings suggested that PAMAM dendrimers might be potentially safe absorption enhancers for improving absorption of FDs by increasing the secretion of OCT1, OCT2, and OCT3.

Characterization of human insulin microcrystals and their absorption enhancement by protease inhibitors in rat lungs

2007 ◽  
Vol 339 (1-2) ◽  
pp. 205-212 ◽  
Author(s):  
Sang-Ha Park ◽  
Jai-Hyun Kwon ◽  
Se-Hwan Lim ◽  
Hye Won Park ◽  
Chan-Wha Kim
Keyword(s):  
Protease Inhibitors ◽  
Human Insulin ◽  
Absorption Enhancement ◽  
Rat Lungs

SEM of non-coated hepatocellular cytoskeleton of perfused livers

1984 ◽  
Vol 42 ◽  
pp. 306-307
Author(s):  
S.W. French ◽  
N.C. Benson ◽  
C. Davis-Scibienski
Keyword(s):  
Ambient Temperature ◽  
Critical Point ◽  
Protease Inhibitors ◽  
Metal Deposition ◽  
Heat Damage ◽  
Detergent Extraction ◽  
Cytoskeletal Elements ◽  
Triton X ◽  
Excised Tissue

Previous SEM studies of liver cytoskeletal elements have encountered technical difficulties such as variable metal coating and heat damage which occurs during metal deposition. The majority of studies involving evaluation of the cell cytoskeleton have been limited to cells which could be isolated, maintained in culture as a monolayer and thus easily extracted. Detergent extraction of excised tissue by immersion has often been unsatisfactory beyond the depth of several cells. These disadvantages have been avoided in the present study. Whole C3H mouse livers were perfused in situ with 0.5% Triton X-100 in a modified Jahn's buffer including protease inhibitors. Perfusion was continued for 1 to 2 hours at ambient temperature. The liver was then perfused with a 2% buffered gluteraldehyde solution. Liver samples including spontaneous tumors were then maintained in buffered gluteraldehyde for 2 hours. Samples were processed for SEM and TEM using the modified thicarbohydrazide procedure of Malich and Wilson, cryofractured, and critical point dried (CPD). Some samples were mechanically fractured after CPD.

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