Design, Formulation, and Characterization of Stearic Acid-Based Solid Lipid Nanoparticles of Candesartan Cilexetil to Augment Its Oral Bioavailability

Mahajan, Anu; Kaur, Satvinder

doi:10.22159/ajpcr.2018.v11i4.23849

Cited by 20 publications

(26 citation statements)

References 30 publications

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“…fig. (8) and (9) show the DSC results for dispersions prepared with aerosil ® 200 and sylysia ® It is obvious from ( fig. (8) that solid dispersions prepared with aerosil 350, respectively.…”

Section: Resultsmentioning

confidence: 94%

“…According to the classical Noyes-Whitney equation, this will increase the dissolution rate [3] One way to increase the surface area to improve the dissolution rate is by reducing the particle size using micronization. Alternatively, the dissolution rate of (CAN) can be improved also by increasing its aqueous solubility through formation of a cyclodextrin inclusion complex [4] or through the preparation of self-micro emulsifying drug delivery systems (SMEDDS) [5][6][7] or by developing (CAN)-loaded solid lipid nanoparticles (CLNs) [8,9] or through formation of solid dispersion involving effective P-gp inhibition (P-glycoprotein-which is an efflux pump distributed throughout the body especially in the , and is responsible for limiting cellular uptake and the distribution of xenobiotics by pumping any them back into the intestinal lumenfor optimal drug delivery [10,11].…”

Section: Introductionmentioning

confidence: 99%

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Enhancement of Dissolution and Stability of Candesartan Cilexetil–loaded Silica Polymers

2019

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Objective: To prepare stable amorphous solid dispersions of candesartan cilexetil (CAN) with different types of silica, including non-porous (aerosil 200) and porous silica (sylysia 350) using the spray-drying method. Methods: various ratios of candesartan cilexetil (CAN) were spray dried with aerosil and sylysia. Powder x-ray diffraction (x-ray) differential scanning calorimetry (DSC), SEM were used to characterize the spray dried powders in addition to dissolution and stability studies. Results: X-ray results showed that the spray–dried (CAN) in the prepared solid dispersion were in amorphous form irrespective of the used silica. In (DSC) analysis, the melting peak of spray-dried (CAN-silica) solid dispersion disappeared. Dissolution property of (CAN) was remarkably improved by formulating with silica particles. In comparing the effect of the type of the silica particles, the dissolution rate of (CAN) from the spray-dried (CAN-sylysia) was faster than that (CAN-aerosil 200) irrespective of the drug content. It was also shown that the spray-dried formulation with silica did not recrystallize when storing at severe storage conditions (40 °C, 75% RH) for three months, while spray-dried (CAN) without silica easily re-crystallized under the same conditions. Conclusion: Spray drying of (CAN) with sylysia 350 is an efficient method to enhance the dissolution and stability of the drug.

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Section: Resultsmentioning

confidence: 94%

Section: Introductionmentioning

confidence: 99%

Enhancement of Dissolution and Stability of Candesartan Cilexetil–loaded Silica Polymers

2019

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“…So, the combined effect of both electrostatic and steric stabilization is expected in the SLN formulations 72 . In previous studies, it was found that due to the carboxyl group of stearic acid the formulation which contains stearic acid as the lipid phase has shown negative values of zeta potential 67 .…”

Section: Fig 1: Types Of Nanocarriermentioning

confidence: 99%

Untitled

2019

IJPSR

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Nanotechnology has brought about a significant change in the drug delivery system. A plethora of BCS class II drugs are formulated as solid lipid nanoparticles (SLN) due to its poor solubility and bioavailability and has potential applications in drug delivery system. The formulation of SLN involves use of a different type of surfactants and lipids in different concentrations which has shown a greater impact on various physicochemical parameters such as entrapment efficiency, drug release, particle size, zeta potential, storage and stability of the drug. Apart from its unique size-dependent property, merits and demerits, different excipients characterization technique, scale up, storage and stability are reviewed. INTRODUCTION: Nanotechnology has shown a wide range of applications in drug delivery, diagnostics, prognostics and in treatment of diseases. It is an emerging branch with an enormous scope which makes the drug targeting more specific in the form of different type of nanoparticles 1, 2. Nanoparticles may be defined as solid particles with a size range of 10-1000 nm in which the drug can be dissolved, encapsulated, entrapped or attached 3, 4. Solid lipid nanoparticles are prepared from lipids which are solid at room temperature and body temperature 5. These comprise of lipid which is biocompatible such as compritol 888, Cetyl alcohol, stearic acid, glyceryl monooleate (GMO), tripalmitin/dynasan, tristearin/ dynasan, etc. and surfactant for emulsification. These are the nanoparticles which have a small size, large surface area, high drug loading capacity QUICK RESPONSE CODE

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“…The dissolution rates for the prepared microsponges formulae were carried out using USP paddle method at 50 rpm in 900 ml of phosphate buffer H 6.8 containing 0.35% w/v Tween 20 as a dissolution media, maintained at 37±0.5°C. The samples were collected at specified time intervals (5,10,15,20,25, and 30 min), filtered through Whatmann filter paper and assayed spectrophotometrically at 254 nm. An equal volume of fresh medium, which was pre-warmed at 37°C, was replaced into the dissolution media after each sampling to maintain a constant volume throughout the test [13,14].…”

Section: In Vitro Dissolution Studymentioning

confidence: 99%

“…CC is a highly lipophilic compound. Therefore, it is necessary to find a new approach to enhance the oral bioavailability of the drug [5].…”

Section: Introductionmentioning

confidence: 99%

Enhancement of the Solubility and the Dissolution Rate of Candesartan Cilexetil Using Microsponge Technology

Alhammid

2018

Asian J Pharm Clin Res

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Objective: The aim of the present study is to enhance the dissolution rate of candesartan cilexetil (CC) using microsponges. Candesartan is therapeutically a potent antihypertensive agent, but it suffers a major drawback of poor oral bioavailability, which is estimated to be 15% due to its low solubility in the gastrointestinal fluids and hepatic first-pass metabolism.Methods: Eudragit-based microsponges were prepared by quasi-emulsion solvent diffusion method using different drug–polymer ratios (1:1 to 1:6), stirring speeds (250–750 rpm), and emulsifier concentrations (polyvinyl alcohol) (0.05%–0.083% w/v). Differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR) study for CC, physical mixtures of drug–polymer, and selected formula were investigated to estimate compatibility of CC with other used ingredients. All formulations were evaluated for particle size, production yield, and loading efficiency. The in vitro drug release study of optimized formulation was performed in phosphate buffer pH 6.8.Results: The obtained results indicated that formula F3 which contains eudragit RS100 at drug:polymer ratio (6:1) was showed the smallest particle size with higher production yield and loading efficiency. DSC and FTIR study of the physical mixtures of drug and polymer revealed no drug–polymer interaction. The results clearly confirm that the percentage of CC released at 30 min from F3, CC powder, and self-made tablet was 54%, 20.325, and 38.9%, respectively.Conclusion: Microsponges technique was considered as a promising system to enhance the solubility and dissolution rate of poor-water soluble CC.

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Design, Formulation, and Characterization of Stearic Acid-Based Solid Lipid Nanoparticles of Candesartan Cilexetil to Augment Its Oral Bioavailability

Cited by 20 publications

References 30 publications

Enhancement of Dissolution and Stability of Candesartan Cilexetil–loaded Silica Polymers

Enhancement of Dissolution and Stability of Candesartan Cilexetil–loaded Silica Polymers

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Enhancement of the Solubility and the Dissolution Rate of Candesartan Cilexetil Using Microsponge Technology

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