Preparation and in vitro-in vivo evaluation of acyclovir floating tablets

Najafi, Rahim Bahri; Mostafavi, Abolfazl; Tavakoli, Naser; Taymouri, Somayeh; Shahraki, Mohammad-Mehdi

doi:10.4103/1735-5362.202451

Cited by 23 publications

(18 citation statements)

References 15 publications

(14 reference statements)

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“…Acquity ultra performance liquid chromatographic system (Waters, MA USA) with UV detection set at 254 nm was used to quantify the concentration of acyclovir in plasma as described by previous studies [ 26 , 27 ]. UPLC was equipped with a photodiode array (PDA) detector and a quaternary solvent delivery system.…”

Section: Methodsmentioning

confidence: 99%

Acyclovir-Loaded Solid Lipid Nanoparticles: Optimization, Characterization and Evaluation of Its Pharmacokinetic Profile

et al. 2020

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Acyclovir is an antiviral drug used for the treatment of herpes simplex virus infection. Its oral bioavailability is low; therefore, frequent and high doses are prescribed for optimum therapeutic efficacy. Moreover, the current therapeutic regimen of acyclovir is associated with unwarranted adverse effects, hence prompting the need for a suitable drug carrier to overcome these limitations. This study aimed to develop solid lipid nanoparticles (SLNs) as acyclovir carriers and evaluate their in vivo pharmacokinetic parameters to prove the study hypothesis. During the SLN development process, response surface methodology was exploited to optimize the composition of solid lipid and surfactant. Optimum combination of Biogapress Vegetal 297 ATO and Tween 80 was found essential to produce SLNs of 134 nm. The oral bioavailability study showed that acyclovir-loaded SLNs possessed superior oral bioavailability when compared with the commercial acyclovir suspension. The plasma concentration of acyclovir-loaded SLNs was four-fold higher than the commercial suspension. Thus, this investigation presented promising results that the method developed for encapsulation of acyclovir offers potential as an alternative pathway to enhance the drug’s bioavailability. In conclusion, this study exhibited the feasibility of SLNs as an oral delivery vehicle for acyclovir and therefore represents a new promising therapeutic concept of acyclovir treatment via a nanoparticulate drug delivery system.

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Section: Methodsmentioning

confidence: 99%

Acyclovir-Loaded Solid Lipid Nanoparticles: Optimization, Characterization and Evaluation of Its Pharmacokinetic Profile

et al. 2020

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“…An Acquity ultra-performance liquid chromatographic system (Waters, Milford, MA, USA) was used to measure the estimated concentration of acyclovir in the plasma samples following the method in previous studies [ 56 , 57 ]. The UPLC was equipped with a photodiode array (PDA) detector and a quaternary solvent delivery system.…”

Section: Methodsmentioning

confidence: 99%

Central Composite Design for Formulation and Optimization of Solid Lipid Nanoparticles to Enhance Oral Bioavailability of Acyclovir

et al. 2021

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Treatment of herpes simplex infection requires high and frequent doses of oral acyclovir to attain its maximum therapeutic effect. The current therapeutic regimen of acyclovir is known to cause unwarranted dose-related adverse effects, including acute kidney injury. For this reason, a suitable delivery system for acyclovir was developed to improve the pharmacokinetic limitations and ultimately administer the drug at a lower dose and/or less frequently. In this study, solid lipid nanoparticles were designed to improve the oral bioavailability of acyclovir. The central composite design was applied to investigate the influence of the materials on the physicochemical properties of the solid lipid nanoparticles, and the optimized formulation was further characterized. Solid lipid nanoparticles formulated from Compritol 888 ATO resulted in a particle size of 108.67 ± 1.03 nm with an entrapment efficiency of 91.05 ± 0.75%. The analyses showed that the optimum combination of surfactant and solid lipid produced solid lipid nanoparticles of good quality with controlled release property and was stable at refrigerated and room temperature for at least 3 months. A five-fold increase in oral bioavailability of acyclovir-loaded solid lipid nanoparticles was observed in rats compared to commercial acyclovir suspension. This study has presented promising results that solid lipid nanoparticles could potentially be used as an oral drug delivery vehicle for acyclovir due to their excellent properties.

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“…It was a modified method 7 described by Bahri-Najafi et al, 2003. Three batches (F1, F2, F3) were prepared with 1:3 ratio of other polymer (carbopol/ tragacanth/sodium alginate) and HPMC K4M.…”

Section: Methodsmentioning

confidence: 99%

“…The moisture gain for CP934 is significantly higher compared to moisture gain for HPMC (55% weight gain for CP934 versus ∼33% for HPMC at RH of 95%); this results in a dramatic increase in the density of the GFDDS, which, in turn, shows a corresponding decrease in the floating capacity of GFDDS. CP934, a polyacrylic acid-based system, appears to have a much stronger solid water interaction compared with HPMC, a cellulosebased polymer 7 . Further, the investigated gastric floating systems employed sodium bicarbonate (NaHCO 3 ) as a gas-forming agent, which is trapped in a hydrogel matrix (HPMC K 4 M and Na alginate).…”

Section: Fig 1: Standard Curve Of Apremilastmentioning

confidence: 99%

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2021

IJPSR

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Apremilast, the new PDE4 inhibitor drug, exhibits low solubility and low permeability; therefore, shows variable bioavailability. Effervescent floating tablets of apremilast were developed to sustain the drug release rate by increasing gastric retention time. These tablets were prepared by wet granulation technique, using different polymers like carbopol 934P, hydroxypropyl methylcellulose K4M, tragacanth and sodium alginate, either alone or in combination. Prepared tablets were characterized for physical parameters like floating capacity, hardness, % weight variation, friability, and content uniformity. Additionally, tablets were evaluated for in vitro release characteristics for 24 h. Results of this study exhibited good physical properties within the limit of acceptance. Batches prepared by carbopol 934P did not show any initial burst release as compared to other polymers. When polymer concentrations were increased drug release rate was decreased. Drug release from the tablets was followed by zero-order controlled release. Sodium alginate/ tragacanth and HPMC K4 in 1:3 ratio exhibited best drug release for 24 h. Carbopol batches (1:3 ratio ) showed very first floating lag time (52 S) but less total floating time (only 8 hrs). However, formulations F5 and F6 (1:7) ratio showed total floating time more than 22 h. From this study we conclude that floating tablets enhance and sustained apremilast release time and would be considered for further in-vivo study. INTRODUCTION:A new (approved by the FDA in 2014) small molecule apremilast (APM), an inhibitor of type-4 cyclic nucleotide phosphor di esterase (PDE-4) is a promising candidate in the treatment of active psoriatic arthritis and plaque psoriasis in adult. PDE-4 is predominantly found in inflammatory cells. Therefore the mechanism of this drug is to inhibit PDE-4 so that intracellular levels of cAMP increase and thereby inhibit the production of multiple pro-inflammatory mediators. Chemically it is a phthalimide derivative and nonhygroscopic in nature.

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Preparation and in vitro-in vivo evaluation of acyclovir floating tablets

Cited by 23 publications

References 15 publications

Acyclovir-Loaded Solid Lipid Nanoparticles: Optimization, Characterization and Evaluation of Its Pharmacokinetic Profile

Acyclovir-Loaded Solid Lipid Nanoparticles: Optimization, Characterization and Evaluation of Its Pharmacokinetic Profile

Central Composite Design for Formulation and Optimization of Solid Lipid Nanoparticles to Enhance Oral Bioavailability of Acyclovir

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