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 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 Comparative in vivo study of pure drug and fast dissolving tablets of Simvastatin

2019 ◽  
Vol 9 (4-A) ◽  
pp. 490-496
Author(s):  
M. Suresh Babu ◽  
T. E. Gopalakrishna Murthy
Keyword(s):  
Rate Constant ◽  
Plasma Levels ◽  
Peak Plasma ◽  
Peak Plasma Concentration ◽  
Elimination Rate ◽  
In Vivo Studies ◽  
Pharmacokinetic Parameters ◽  
Pharmacokinetic Studies ◽  
Pure Drug

The objective of this study was to investigate differences in the pharmacokinetic patterns between pure drug and an optimized  formulation of fast dissolving tablets  of Simvastatin. The formulations were administered to 2 groups of white New Zealand rabbits (n=6) following cross over design pattern and the plasma levels were measured using LC-MS/MS method. Pharmacokinetic parameters were determined for each formulation. The comparison of the plasma time curves of the dosage forms showed that each dosage form caused significant differences in the drug plasma levels.  The highest mean Cmax value was observed for optimized fast dissolving tablets (68.33 ± 0.42ng/ml) compared to  pure drug (27.72 ± 0.31ng/ml). The mean time taken to peak plasma concentration for (Tmax) following administration of pure drug  was  11.53 ± 0.011hours, while it was 6.09 ± 0.072 hour following administration of selected optimized fast dissolving tablets.The elimination rate constant (Kel) for pure drug and optimized fast dissolving tablets were found to be 0.58 ± 0.012h-1and 0.53 ± 0.014 h-1 respectively.  The absorption rate constant (Ka) for pure drug and optimized fast dissolving tablets were found to be 1.68 ± 0.01h-1and 5.53 ± 0.02h-1 respectively. The AUC0-αvalues observed with optimized fast dissolving tablets686.1.±2.07 nghr/ml in compared to pure drug values 191 ± 1.43 nghr/ml. Thus, the results of pharmacokinetic studies indicated rapid and higher oral absorption of Simvastatin when administered as its fast dissolving tablets. Both Ka and AUC were markedly increased by fast dissolving tablets. Keywords: LC-MS/MS, Simvastatin, fast dissolving, In-vivo studies, pharmacokinetic parameters.

scholarly journals In vitro–in vivo and pharmacokinetic evaluation of solid lipid nanoparticles of furosemide using Gastroplus™

RSC Advances ◽  
2017 ◽  
Vol 7 (53) ◽  
pp. 33314-33326 ◽  
Author(s):  
Hasan Ali ◽  
Priya Ranjan Prasad Verma ◽  
Sunil Kumar Dubey ◽  
Jayachandran Venkatesan ◽  
Youngwan Seo ◽  
...  
Keyword(s):  
Solid Lipid Nanoparticles ◽  
Lipid Nanoparticles ◽  
Pharmacokinetic Studies ◽  
Solid Lipid ◽  
Pharmacokinetic Evaluation

In this work, we conducted pharmacokinetic studies and established the in vitro and in vivo correlation (IVIVC) of furosemide (FRS) loaded solid lipid nanoparticles (FSLN).

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 Design and in vivo Evaluation of Manidipine by Self-Nanoemulsifying Drug Delivery Systems

2019 ◽  
Vol 11 (06) ◽  
Author(s):  
S Srikanth Reddy ◽  
G Suresh
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Release ◽  
Spherical Shape ◽  
Pharmacokinetic Studies ◽  
In Vivo Evaluation ◽  
Enhanced Solubility ◽  
Pure Drug

The current research is aimed at developing liquid self-nanoemulsifying drug delivery system (liquid-SNEDDS) of Manidipine for enhanced solubility and oral bioavailability. The Manidipine SNEDDS are formulated with excipients comprising of Capmul MCM (oil phase), Transcutol P (surfactant) Lutrol L 300 as co-surfactant. The prepared fifteen formulations of Manidipine SNEDDS analysed for emulsification time, percentage transmittance, particle size, in vitro drug release, and stability studies. In vivo pharmacokinetic studies of the optimized formulation were carried out in Wistar rats in comparison with control (pure drug). The morphology of Manidipine SNEDDS indicates spherical shape with uniform particle distribution. The percentage drug release from optimized formulation F14 is 98.24 ± 5.14%. The particle size F14 formulation was 22.4 nm and Z-Average 23.3 nm. The PDI and zeta potential of Manidipine SNEDDS optimized formulation (F14) were 0.313 and-5.1mV respectively. From in vivo bioavailability data the optimized formulation exhibited a significantly greater Cmax and Tmax of the SNEDDS was found to be 3.42 ± 0.46ng/ml and 2.00 ± 0.05 h respectively. AUC0-∞ infinity for formulation was significantly higher (11.25 ± 3.45 ng.h/ml) than pure drug (7.45 ± 2.24ng. h/ml). Hence a potential SNEDDS formulation of Manidipine developed with enhanced solubility and bioavailability.

Lacidipine Loaded Solid Lipid Nanoparticles for Oral Delivery: Preparation, Characterization and In vivo Evaluation

2016 ◽  
Vol 9 (6) ◽  
pp. 3524-3530 ◽  
Author(s):  
Kishan V. ◽  
Sandeep V ◽  
Narendar D ◽  
Arjun N
Keyword(s):  
Solid Lipid Nanoparticles ◽  
Oral Bioavailability ◽  
Oral Delivery ◽  
Lipid Nanoparticles ◽  
Pharmacokinetic Studies ◽  
Electron Microscopic ◽  
In Vivo Evaluation ◽  
Solid Lipid

The objective of this study was to develop and evaluate lacidipine (LD) loaded solid lipid nanoparticles (LD-SLNs) for improving the oral bioavailability. LD-SLNs were prepared in two steps. First step was hot homogenization and next by ultrasonication method, using triglycerides (tripalmitin and tristearin), monoglyceride and surfactants (Poloxamer 188 and egg lecithin E80). The prepared LD-SLNs were characterized for particle size, PDI, zeta potential, drug content, entrapment efficiency (EE %).         In vitro drug release studies using a dialysis bag method in 0.1N HCl and pH 6.8 phosphate buffer were conducted. In addition, long-term physical stability of the optimized SLNs was investigated at refrigerated and room temperature for 60 days. FTIR and DSC studies revealed that no interaction between the drug and lipids. LD-SLNs prepared with Dynasan-116 (F3), having the size of 141.86nm, PDI of 0.293, ZP of -22.3 m with 94.75% of EE was optimized and was stable for 60days. Scanning electron microscopic studies showed nearly spherical shaped particles. Further, pharmacokinetic studies were conducted in wistar rats. The relative bioavailability of LD in SLNs was 2.03 times when compared with that of the LD suspension. The results are indicative of SLNs as suitable lipid based carrier system for improving the oral bioavailability of LD. 

scholarly journals Fabrication, Characterization, and In Vivo Evaluation of Famotidine Loaded Solid Lipid Nanoparticles for Boosting Oral Bioavailability

2017 ◽  
Vol 2017 ◽  
pp. 1-10 ◽  
Author(s):  
Muhammad Shafique ◽  
Mir Azam Khan ◽  
Waheed S. Khan ◽  
Maqsood-ur-Rehman ◽  
Waqar Ahmad ◽  
...  
Keyword(s):  
Drug Release ◽  
Solid Lipid Nanoparticles ◽  
Oral Bioavailability ◽  
Lipid Nanoparticles ◽  
Fickian Diffusion ◽  
Release Time ◽  
Pharmacokinetic Studies ◽  
Prolonged Release ◽  
Solid Lipid

Famotidine as H2 receptor has antagonistic effects on gastric secretion. Unfortunately, its hydrophobic nature contributes to its variable and poor oral bioavailability. In the current study efforts are being made to fabricate famotidine loaded solid lipid nanoparticles with narrow size distribution. Prepared nanoformulations were pharmaceutically evaluated to confirm the desired boosted oral bioavailability. Famotidine loaded nanoformulation (FFSe-4) showed particle size 111.9±1.3 nm, polydispersity index 0.464±0.03, zeta potential −33.46±2 mV, entrapment efficiency 84±2.7%, and drug loading capacity 2.709±0.13%. Drug-excipients compatibility was confirmed by Fourier transformed infrared spectroscopy. Scanning electron microscopy confirmed spherical shaped, nanosized particles. Differential scanning calorimetry and powder X-ray diffractometry confirmed the change in crystalline nature. Prepared nanoformulation was more stable at refrigerated temperature. In vitro study showed that drug release time is proportional to drug pay load and followed zero order kinetics. Release exponent (n>0.5) confirmed non-Fickian-diffusion mechanism for drug release. In vivo pharmacokinetic studies showed 2.06-fold increase in oral bioavailability of famotidine dispersed in solid lipid nanoparticles compared to commercial product. These results authenticate solid lipid nanoparticles as drug delivery system and propose prolonged release with improved oral bioavailability for famotidine.

scholarly journals Cytotoxicity and Biological Efficacy of Exendin-4-Encapsulated Solid Lipid Nanoparticles in INS-1 Cells

2015 ◽  
Vol 2015 ◽  
pp. 1-6 ◽  
Author(s):  
Hee-Sook Jun ◽  
Gongdeuk Bae ◽  
Young Tag Ko ◽  
Yoon Sin Oh
Keyword(s):  
Solid Lipid Nanoparticles ◽  
Biological Effects ◽  
Lipid Nanoparticles ◽  
Pharmacokinetic Studies ◽  
Mrna Levels ◽  
Solid Lipid ◽  
Vehicle Treatment ◽  
Glucagon Like Peptide 1

Exendin-4 (Ex-4), a peptide of glucagon-like peptide-1 receptor agonist, is a potent insulinotropic agent and alternative drug delivery systems to increase therapeutic utility have been explored. We developed exendin-4-encapsulated solid lipid nanoparticles (Eudragit Ex-4 SLNs) and compared the effects of Eudragit Ex-4 SLNs with those of native Ex-4 on INS-1 cells. We observed no significant toxic effects of nanoparticles at concentrations from 1 nM to 100 nM. Similar to Ex-4, Eudragit Ex-4 SLNs stimulated the production of cyclic AMP at 10 nM. Moreover, unlike treatment with the vehicle, treatment with 10 nM Eudragit Ex-4 SLNs increased insulin mRNA levels and insulin secretion. These insulinotropic effects of Eudragit Ex-4 SLNs were comparable to those of Ex-4. Thus, ourin vitroresults suggest that the biological effects of Eudragit Ex-4 SLNs are similar to those of Ex-4, and furtherin vivopharmacokinetic studies are required to propose an alternative sustained release drug system.

Licochalcone A-loaded solid lipid nanoparticles improve antischistosomal activity in vitro and in vivo

Nanomedicine ◽  
2021 ◽  
Author(s):  
Lívia Mara Silva ◽  
Danielle Gomes Marconato ◽  
Marcos Paulo Nascimento da Silva ◽  
Nádia Rezende Barbosa Raposo ◽  
Gabriela de Faria Silva Facchini ◽  
...  
Keyword(s):  
Solid Lipid Nanoparticles ◽  
Lipid Nanoparticles ◽  
Homogenization Method ◽  
Licochalcone A ◽  
Solid Lipid ◽  
Transmission Electron ◽  
High Shear Homogenization ◽  
Antischistosomal Activity

Aim: To isolate licochalcone A (LicoA) from licorice, prepare LicoA-loaded solid lipid nanoparticles (L-SLNs) and evaluate the L-SLNs in vitro and in vivo against Schistosoma mansoni. Materials & methods: LicoA was obtained by chromatographic fractionation and encapsulated in SLNs by a modified high shear homogenization method. Results: L-SLNs showed high encapsulation efficiency, with satisfactory particle size, polydispersity index and Zeta potential. Transmission electron microscopy revealed that L-SLNs were rounded and homogenously distributed. Toxicity studies revealed that SLNs decreased the hemolytic and cytotoxic properties of LicoA. Treatment with L-SLNs showed in vivo efficacy against S. mansoni. Conclusion: L-SLNs are efficient in reducing worm burden and SLNs may be a promising delivery system for LicoA to treat S. mansoni infections.

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