Development and characterization of Solid-SNEDDS formulation of DHA using hydrophilic carrier with improved shelf life, oxidative stability and therapeutic activity

Singh, Harmanpreet; Nathani, Sandip; Singh, Narpinder; Roy, Partha; Paul, Surinder; Sohal, Harminder Singh; Jain, Subheet Kumar

doi:10.1016/j.jddst.2019.101326

Cited by 19 publications

(21 citation statements)

References 35 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The external morphological structure for pure LMG, Aeroperl ® 300, their PM, and the optimized S-SNEDDS was done using SEM (SEM, Model Quanta 250 FEG, FEI Company, Eindhoven, Netherlands) attached with EDX unit (Energy Dispersive X-ray Analyses), with accelerating voltage 30 kV. 49 …”

Section: Methodsmentioning

confidence: 99%

<p>Development, Characterization, and in-vivo Pharmacokinetic Study of Lamotrigine Solid Self-Nanoemulsifying Drug Delivery System</p>

Abdelmonem

Azer

Makky

et al. 2020

DDDT

View full text Add to dashboard Cite

This study aimed to prepare solid self-nanoemulsified drug delivery system (S-SNEDDS) of lamotrigine (LMG) for enhancing its dissolution and oral bioavailability (BA). Methods: Nineteen liquid SNEDDS were prepared (R1-R19) using D-optimal design with different ratios of oil, surfactant (S), and cosurfactant (Cos). The formulations were characterized regarding robustness to dilution, droplet size, thermodynamic stability testing, selfemulsification time, in-vitro release in 0.1 N HCl and phosphate buffer (PB; pH 6.8). Design Expert ® 11 software was used to select the optimum formulations. Eight S-SNEDDS were prepared (S1-S8) using 2 3 factorial design, and characterized by differential scanning calorimetry (DSC), powder x-ray diffraction (PXRD), and scanning electron microscopy (SEM). The optimum formulation was chosen regarding in-vitro drug released in 0.1 N HCl and PB, compared to pure LMG and commercial tablet (Lamictal ®). The BA of LMG from the optimized S-SNEDDS formulation was evaluated in rabbits compared to pure LMG and Lamictal ®. Results: The optimized S-SNEDDS was S2, consisting of R9 adsorbed on Aeroperl ® 300 in a ratio of 1:1, with the best results regarding in-vitro drug released in 0.1 N HCl at 15 min (100%) compared to pure LMG (73.40%) and Lamictal ® (79.43%), and in-vitro drug released in PB at 45 min (100%) compared to pure LMG (30.46%) and Lamictal ® (92.08%). DSC, PXRD, and SEM indicated that LMG was molecularly dispersed within the solid nano-system. The BA of S2 was increased 2.03 and 1.605 folds compared to pure LMG, and Lamictal ® , respectively. Conclusion: S2 is a promising S-SNEDDS formulation. It can be a potential carrier for improving dissolution, and BA of LMG.

show abstract

Section: Methodsmentioning

confidence: 99%

<p>Development, Characterization, and in-vivo Pharmacokinetic Study of Lamotrigine Solid Self-Nanoemulsifying Drug Delivery System</p>

Abdelmonem

Azer

Makky

et al. 2020

DDDT

View full text Add to dashboard Cite

show abstract

“…Pharmacodynamic evaluation of change in memory episodes was done with Morris water maze (MWM) and Rotarod tests. 61 4.6.4.2. Morris Water Maze Test.…”

Section: Methodsmentioning

confidence: 99%

“…The time taken for mice to enter the platform was measured as the escape latency (EL) at day 0 (starting), 28 (after cognitive impairment with melamine), and 56 (after treatment with donepezil and 4b molecules). 61,62 4.6.4.3. Behavioral and Biochemical Estimations.…”

Section: Methodsmentioning

confidence: 99%

Donepezil-Inspired Multitargeting Indanone Derivatives as Effective Anti-Alzheimer’s Agents

Singh

Thakur

Kumar

et al. 2022

ACS Chem. Neurosci.

View full text Add to dashboard Cite

In continuous efforts to develop anti-Alzheimer’s agents, we rationally designed and synthesized a series of multitargeting molecules by incorporating the essential molecular features of the standard drug donepezil. Among the series, compound 4b showed multitargeting properties to act as an anti-Alzheimer’s agent, which is better tolerable in vivo than donepezil. Acetylcholinesterase (AChE) inhibition data showed that compound 4b inhibits the enzyme with a half-maximal inhibitory concentration (IC50) value of 0.78 μM and also showed DNA protection, which was confirmed through the DNA nicking assay, suggesting the protective effect of 4b against oxidative DNA damage. Compound 4b also showed 53.04% inhibition against Aβ1–42 aggregations, which was found comparable to that of the standard compound curcumin. Molecular dynamics simulations were performed to check the stability of compound 4b with the enzyme AChE, which showed that the enzyme–ligand complex is stable enough to block the hydrolysis of acetylcholine in the brain. Its higher LD50 cutoff value (50 mg/kg) in comparison to donepezil (LD50: 25 mg/kg) made it safer, suggesting that it can be used in further clinical experiments. To evaluate its anti-Alzheimer property, a mice model with melamine-induced cognitive dysfunction was used, and Morris water maze and Rotarod tests were performed. A significant improvement in memory was observed after the treatment with compound 4b and donepezil. The study postulated that the introduction of important structural features of donepezil (dimethoxyindanone moiety as ring-A) embarked with terminal aromatic ether (ring-B and ring-C) made 4b a multitargeting molecule that offers a way for developing alternative therapeutics in the future against Alzheimer’s disease (AD).

show abstract

“…The SNEDDS method produces small round particles with oxidative stability and that are free-flowing, so they can be developed as solid dosage forms [61]. SNEDDS is also a promising carrier because it improves the bioavailability and therapeutic effects of the class II BCS drugs [62].…”

Section: Sneddsmentioning

confidence: 99%

Methods for Improving Alpha-Mangostin Solubility: A Review

2021

View full text Add to dashboard Cite

Solubility is an important parameter to achieve for the bioavailability of a drug to reach the therapeutic windows. Garcinia mangostana Linn is a plant with great potency for the development of natural medicine. Alpha-mangostin is one of the secondary metabolites of G. mangostana and has been reported to have several pharmacological activities. The Biopharmaceutics Classification System (BCS) is a system that classifies drugs based on their solubility and permeability. Due to its low solubility but high permeation, alpha-mangostin is categorized into class II of the Biopharmaceutics Classification System. Therefore, the determination of dosage forms and modification of solubility enhancers is limited due to its physical properties, as mentioned above. This disadvantage requires new methods to improve its solubility to administer alpha-mangostin, especially for oral administration. Here, we discuss the development of the methods to increase alpha-mangostin solubility to be applied to formulate a dosage form to reach a useful plasma level for medication.

show abstract

Development and characterization of Solid-SNEDDS formulation of DHA using hydrophilic carrier with improved shelf life, oxidative stability and therapeutic activity

Cited by 19 publications

References 35 publications

<p>Development, Characterization, and in-vivo Pharmacokinetic Study of Lamotrigine Solid Self-Nanoemulsifying Drug Delivery System</p>

<p>Development, Characterization, and in-vivo Pharmacokinetic Study of Lamotrigine Solid Self-Nanoemulsifying Drug Delivery System</p>

Donepezil-Inspired Multitargeting Indanone Derivatives as Effective Anti-Alzheimer’s Agents

Methods for Improving Alpha-Mangostin Solubility: A Review

Contact Info

Product

Resources

About