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

Abstract

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.

Dexamethasone-Loaded Nanostructured Lipid Carriers for the Treatment of Dry Eye Disease

“…The intermediate positive charge observed for this pilot scale formulation, +9.8 mV, is postulated to be due to the presence of the Tween 80 layer. Similar effects have been observed by Hassan et al, where Tween 80 was shown to produce a “less negative” surface charge for solid lipid nanoparticles [ 59 ]. Lason et al also highlight the transition to a positive charge when using Tween 80 alone as a surfactant for NLC formulation, recording an increase to +17.9 mV from a negative −50.1 mV when used with PlantaCare [ 17 ].…”

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

“…These findings could be attributed to the full coverage of the non-ionic surfactant, Tween 80, which causes steric hindrance, as well as electrostatic repulsion from the solid lipid [43]. Surprisingly, this was not the case for SLN that was developed using Biogapress Vegetal 297 ATO as solid lipid material, in our previous study [8]. Although the same methods and optimization processes were employed to develop this nanocarrier system, after the first month of storage, the size of the blank Biogapress Vegetal 297 ATO SLN and acyclovir-loaded Biogapress Vegetal 297 ATO SLN formulations stored at room temperature started to increase significantly, and high polydispersity index values were recorded.…”

“…In the past, various pharmaceutical formulations, such as lipid-based nanoparticles [ 8 ], polymeric nanoparticulate systems [ 9 ], mixed micelles and niosomal carriers [ 10 , 11 ] have been studied as strategies to increase the solubility and bioavailability of poorly soluble drugs. Several attempts have also been made to incorporate acyclovir into different types of delivery systems, including microemulsion [ 12 ], liposome [ 13 ] and nanoemulsion [ 14 ] to enhance its bioavailability [ 6 , 15 ].…”

Application of solid lipid nanoparticles preparation in infection caused by antibiotic-resistant bacteria

“…17 The uptake of SLNs into lymphatic system can occur via two mechanisms: M-cell-mediated uptake and paracellular/transcellular route. 18 Basically, SLN properties such as particle size and shape can affect their bioavailability. Small particles tend to adhere to cell-surface while large particles (>200 nm) are filtered out by reticular meshwork.…”