Formulation and Optimization of Candesartan Cilexetil Nano Lipid Carrier: In Vitro and In Vivo Evaluation

Paudel, Anjan; Ameeduzzafar,; Imam, Syed Sarim; Fazil, Mohd; Khan, Sajjad Ahmad; Hafeez, Abdul; Ahmad, Feroz; Ali, Asgar

doi:10.2174/1567201813666161230141717

Cited by 15 publications

(7 citation statements)

References 0 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The results of the zeta sizer revealed that the average diameter of the nanoparticles was 203.2±0.418 nm and uniform particle size distribution (PDI of 0.189). These results indicated the formation of SE-EE 5 nanoparticles [ 47 ].…”

Section: Resultsmentioning

confidence: 99%

Solid dispersion systems for enhanced dissolution of poorly water-soluble candesartan cilexetil: In vitro evaluation and simulated pharmacokinetics studies

Ali,

Sajad,

Abdul Rasool

2024

PLoS ONE

View full text Add to dashboard Cite

Background Candesartan cilexetil (CC) is a selective angiotensin II receptor antagonist widely used to treat hypertension. CC is a substrate of P-glycoprotein (P-gp), causing its efflux to the intestinal lumen. It is also practically insoluble in water and has low oral bioavailability (14%). Thus, the current study aims to improve the in vitro dissolution of CC by developing solid dispersion systems (SDSs) and corroborating the in vitro results using a simulated pharmacokinetics study. Methods The SDSs were prepared using polyvinyl pyrrolidone (PVP) as a water-soluble polymer, Eudragit E100 (EE100) as a pH-dependent soluble carrier, and a combination of these two polymers. The saturation solubility and the dissolution rate studies of the prepared systems in three dissolution media were performed. The optimized system SE-EE5 was selected for further investigations, including DSC, XRD, FTIR, FESEM, DLS, TSEM, IVIVC convolution study, and stability studies. Results The solubility of CC significantly increased by a factor of 27,037.344 when formulated as a solid dispersion matrix using EE100 at a ratio of 1:5 (w/w) drug to polymer (SE-EE5 SD), compared to the solubility of the pure drug. The mechanism of solubility and dissolution rate enhancement of CC by the optimized SDS was found to be via the conversion of the crystalline CC into the amorphous form as well as nanoparticles formation upon dissolution at a pH below 5. The instrumental analysis tests showed good compatibility between CC and EE100 and there was no chemical interaction between the drug and the polymer. Moreover, the stability tests confirmed that the optimized system was stable after three months of storage at 25°C. Conclusion The utilization of the solid dispersion technique employing EE 100 polymer as a matrix demonstrates significant success in enhancing the solubility, dissolution, and subsequently, the bioavailability of water-insoluble drugs like CC.

show abstract

Section: Resultsmentioning

confidence: 99%

Solid dispersion systems for enhanced dissolution of poorly water-soluble candesartan cilexetil: In vitro evaluation and simulated pharmacokinetics studies

Ali,

Sajad,

Abdul Rasool

2024

PLoS ONE

View full text Add to dashboard Cite

show abstract

“…TQSLN has shown percentage release of about 78.34 ± 5.12 in 24 h, whereas TQS has shown only 30.21% release in same time. The lipophilic nature of the drug could be the reason for sustained release from lipid phase after initial burst release [33]. TQSLN has shown a typical biphasic release pattern with an initial rapid phase followed by a slow sustained phase (data not shown).…”

Section: Differential Scanning Calorimetrymentioning

confidence: 98%

Formulation and evaluation of nano lipid formulation containing CNS acting drug: molecular docking, in-vitro assessment and bioactivity detail in rats

Alam

Najmi

Ahmad

et al. 2018

Artificial Cells, Nanomedicine, and Biotechnology

Self Cite

View full text Add to dashboard Cite

The study performed molecular docking, formulated, characterized thymoquinone (TQ) loaded solid lipid nano particles (TQSLN) and exhibited comparative antidepressant activity. TQ loaded nano lipid formulations were prepared by solvent injection methods and characterize for different in-vitro parameters. The optimized formulation was evaluated for depression using unpredictable chronic mild stress (UCMS) model for a period of six weeks. TQSLN was assessed in modified forced swim test (MFST), tail suspension test (TST), locomotor activity followed by biochemical parameters such as monoaminesand brain derived neurotrophic factor (BDNF). The results of molecular docking study revealed that TQ has shown greater affinity and tighter binding capacity for the active site of neurotransmitter receptors. TQSLN showed nanometric size, optimum zeta potential with high percent encapsulation and lower poly dispersity index (PDI). Transmission electron microscopy (TEM) images showed spherical shape without aggregation and agglomeration of particles. The in-vivo study result revealed that the higher amount of TQ reaches to the target region by showing higher levels of monoamines 5 hydroxytryptamine (5-HT), dopamine (DA) and norepinephrine (NE) as compared to thymoquinone suspension (TQS) in brain. In conclusion, the nano lipid formulation remarkably improved the bio-efficacy of TQ and demonstrated a promising perspective for oral delivery of poorly water-soluble drugs.

show abstract

“…The comparative ex-vivo gut permeation study of the SIT-NPopt and SIT-FS was performed as per the reported method [34]. Both the formulations (each containing 2 mg SIT) were filled in the mucosal side of the intestinal sac and were tightly ligated.…”

Section: Ex-vivo Permeation Studymentioning

confidence: 99%

“…The image was taken using an argon laser beam excitation at 488 nm and emission at 532 nm. The depth of permeation was measured by Leica application suite Advance Fluorescence software [34].…”

Section: Confocal Laser Scanning Microscopy (Clsm)mentioning

confidence: 99%

Formulation of sitagliptin-loaded oral polymeric nano scaffold: process parameters evaluation and enhanced anti-diabetic performance

Jahangir

Khan

Imam

2017

Artificial Cells, Nanomedicine, and Biotechnology

View full text Add to dashboard Cite

show abstract

Formulation and Optimization of Candesartan Cilexetil Nano Lipid Carrier: In Vitro and In Vivo Evaluation

Abstract: Thus, the results of ex vivo permeation, pharmacokinetic study and pharmacodynamics study suggest the potential of CC-NLCs for improved oral delivery.

Cited by 15 publications

References 0 publications

Solid dispersion systems for enhanced dissolution of poorly water-soluble candesartan cilexetil: In vitro evaluation and simulated pharmacokinetics studies

Solid dispersion systems for enhanced dissolution of poorly water-soluble candesartan cilexetil: In vitro evaluation and simulated pharmacokinetics studies

Formulation and evaluation of nano lipid formulation containing CNS acting drug: molecular docking, in-vitro assessment and bioactivity detail in rats

Formulation of sitagliptin-loaded oral polymeric nano scaffold: process parameters evaluation and enhanced anti-diabetic performance

Contact Info

Product

Resources

About