Isoniazid—Loaded Albumin Nanoparticles: Taguchi Optimization Method

Tazhbayev, Yerkeblan; Galiyeva, A.R.; Zhumagalieva, T.S.; Burkeyev, M.Zh.; Karimova, B.N.

doi:10.3390/polym13213808

Cited by 8 publications

(5 citation statements)

References 28 publications

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“…The R 2 value could measure the variation amount around the mean described by the model. This model was found to be high (0.9964), which could indicate the model’s ability to detect about 99% of the variations [ 13 ]. The adequate precision could compare the range of the predicted values to the average prediction error.…”

Section: Resultsmentioning

confidence: 99%

“…The particle size parameter of a drug delivery system could represent a fundamental key in drug transportation through systemic circulation. Nanoparticle systems with small particle sizes and hydrophilic surfaces could easily circulate in the blood over extended periods and sustain the duration of the pharmacological effect [ 13 ]. Rejinold et al [ 37 ] found that an optimal nanoparticle size of 250 nm or lower, combined with highly positive or negative charges on the nanoparticle surface, can prevent rapid clearance by the reticuloendothelial system.…”

Section: Resultsmentioning

confidence: 99%

“…Different initial burst release profiles were found among the studied formulations owing to the difference in the concentrations of the components utilized to prepare the nanoparticles. The burst release could be ascribed to the desorption and the diffusion of carvedilol from the outer surface of the BSA-based nanoparticles [ 13 ], where, the higher the amount of unentrapped carvedilol on the particle’s surface with no complete incorporation into the BSA, the faster the dissolution and the initial burst release of the drug [ 38 ]. Aside from this, continuous and sustained drug release could also be due to the slow carvedilol diffusion across the BSA matrix of the nanoparticle formulations by the solubilization of such carriers, including the degradation and erosion of the BSA.…”

Section: Resultsmentioning

confidence: 99%

“…A standard treatment plan for hypertension requires patients to take medications for several months or years to treat this ailment successfully. These patients may suffer from adverse effects following oral drug administration, such as poor drug solubility, pH variations, low intestinal resorption, and low bioavailability, in addition to those following the frequent drug dosage for a long time [ 13 ]. Hence, a potential drug delivery approach can tackle these problems by using a nano-drug delivery system to provide a sustained release of carvedilol when administered by a route other than the oral one.…”

Section: Introductionmentioning

confidence: 99%

“…The desolvation technique is a widespread procedure for developing BSA-based nanoparticles by which a desolvating agent is utilized to prepare well-defined nanoparticles with the denatured albumin and achieve the formation of spherical matrices. In addition, glutaraldehyde is commonly utilized as a crosslinker to ameliorate the stability of the prepared BSA-based nanoparticles [ 13 ]. This technique has gained a distinct superiority due to its desirable merits, including robustness, reproducibility, simplicity, encapsulation of hydrophilic and lipophilic drugs, and production of nanoparticles of smaller sizes and more controlled release than that of microparticles and liposomes, therefore improving the patient acceptance and compliance.…”

Section: Introductionmentioning

confidence: 99%

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Development of Carvedilol-Loaded Albumin-Based Nanoparticles with Factorial Design to Optimize In Vitro and In Vivo Performance

et al. 2023

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Carvedilol, an anti-hypertensive medication commonly prescribed by healthcare providers, falls under the BCS class II category due to its low-solubility and high-permeability characteristics, resulting in limited dissolution and low absorption when taken orally. Herein, carvedilol was entrapped into bovine serum albumin (BSA)-based nanoparticles using the desolvation method to obtain a controlled release profile. Carvedilol-BSA nanoparticles were prepared and optimized using 32 factorial design. The nanoparticles were characterized for their particle size (Y1), entrapment efficiency (Y2), and time to release 50% of carvedilol (Y3). The optimized formulation was assessed for its in vitro and in vivo performance by solid-state, microscopical, and pharmacokinetic evaluations. The factorial design showed that an increment of BSA concentration demonstrated a significant positive effect on Y1 and Y2 responses with a negative effect on Y3 response. Meanwhile, the carvedilol percentage in BSA nanoparticles represented its obvious positive impact on both Y1 and Y3 responses, along with a negative impact on Y2 response. The optimized nanoformulation entailed BSA at a concentration of 0.5%, whereas the carvedilol percentage was 6%. The DSC thermograms indicated the amorphization of carvedilol inside the nanoparticles, which confirmed its entrapment into the BSA structure. The plasma concentrations of carvedilol released were observable from optimized nanoparticles up to 72 h subsequent to their injection into rats, revealing their longer in vivo circulation time compared to pure carvedilol suspension. This study offers new insight into the significance of BSA-based nanoparticles in sustaining the release of carvedilol and presents a potential value-added in the remediation of hypertension.

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Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Development of Carvedilol-Loaded Albumin-Based Nanoparticles with Factorial Design to Optimize In Vitro and In Vivo Performance

et al. 2023

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Synthesis and physicochemical characterization of rhamnolipid fabricated fucoxanthin loaded bovine serum albumin nanoparticles supported by simulation studies

et al. 2022

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BACKGROUND: Fucoxanthin is a hydrophobic carotenoid with many beneficial biological activities. However, due to low aqueous solubility their clinical efficacy is limited thus leading to poor oral bioavailability. To address this issue, we encapsulated fucoxanthin in rhamnolipid fabricated bovine serum albumin (BSA) loaded nanoparticles (LNPs) for improving solubility dependent bioavailability of fucoxanthin.RESULTS: These synthesized LNPs were characterized by dynamic light scattering (DLS), ultraviolet (UV)-visible spectrophotometry, high-performance liquid chromatography (HPLC), Fourier-transform infrared (FTIR), scanning electron microscopy (SEM), differential scanning calorimetry (DSC). Our results showed that LNPs were spherical in shape with particle size around 180 nm along with positive zeta potential. The encapsulation efficiency and loading efficiency calculated for LNPs were 69.66 ± 1.5% and 14 ± 0.2%, respectively. The antioxidant assay of LNPs indicate high radical scavenging activity compared to pure fucoxanthin. Besides this, our release studies indicates that drug release occur from the matrix of nanocarrier system through diffusion based on concentration. Thus, these findings indicate successful encapsulation of fucoxanthin, with improved solubility thereby leading to increased bioavailability. This nano formulation is derived from components which are FDA approved that could be exploited for encapsulating other vital nutraceutical molecules. CONCLUSION: Overall, our results showed successful synthesis of biodegradable nanocarrier for delivering fucoxanthin supported by molecular docking, molecular dynamics simulation and thermodynamics of free binding energy studies.

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