Encapsulation challenges, the substantial issue in solid lipid nanoparticles characterization

Daneshmand, Sara; Golmohammadzadeh, Shiva; Jaafari, Mahmoud Reza; Movaffagh, Jebrail; Rezaee, Mehdi; Sahebkar, Amirhossein; Malaekeh‐Nikouei, Bizhan

doi:10.1002/jcb.26617

Cited by 46 publications

(29 citation statements)

References 62 publications

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“…Two parameters, the encapsulation efficiency (% EE ) and the drug loading (% DL ), of SP in mPEG-PCL NPs, were quantified indirectly, as reported elsewhere for other drugs [40]. For this, SP-loaded NP suspensions were washed thoroughly to remove residues of free TAβCD and SP, and free SP quantified in the filtrate fraction and the %EE calculated according to Equation (1)%EE = SPNPSPt × 100%where SP NP is the weight of SP in the NPs and SP t is the total weight of SP used in the encapsulation process.…”

Section: Resultsmentioning

confidence: 99%

Enhanced Nanoencapsulation of Sepiapterin within PEG-PCL Nanoparticles by Complexation with Triacetyl-Beta Cyclodextrin

Kuplennik

Sosnik

2019

Molecules

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In this work, we aimed to improve the encapsulation efficiency of sepiapterin (SP), the natural precursor of the essential cofactor tetrahydrobiopterin (BH4) that displays mild water-solubility and a short biological half-life, within methoxy-poly(ethylene-glycol)-poly(epsilon-caprolactone)(mPEG-PCL) nanoparticles (NPs) by means of its complexation and hydrophobization with 2,3,6-triacetyl-β-cyclodextrin (TAβCD). For this, SP/TAβCD complexes were produced by spray-drying of SP/TAβCD binary solutions in ethanol using the Nano Spray Dryer B-90 HP. Dry powders were characterized by differential scanning calorimetry (DSC), Fourier-transform infrared spectroscopy (FTIR), and transmission and scanning electron microscopy (TEM and SEM, respectively) and compared to the pristine components and their physical mixtures (PMs). Next, SP was encapsulated within mPEG-PCL NPs by nano-precipitation of an SP/TAβCD complex/mPEG-PCL solution. In addition to the nano-encapsulation of a preformed complex within the polymeric NPs, we assessed an alternative encapsulation approach called drying with copolymer (DWC) in which pristine SP, TAβCD, and mPEG-PCL were co-dissolved in a mixture of acetone and methanol at the desired weight ratio, dried under vacuum, re-dissolved, and nano-precipitated in water. The dissolution-drying step was aimed to promote the formation of molecular hydrophobic interactions between SP, TAβCD, and the PCL blocks in the copolymer. SP-loaded mPEG-PCL NPs were characterized by dynamic light scattering (DLS) and SEM. NPs with a size of 74–75 nm and standard deviation (S.D., a measure of the peak width) of 21–22 nm were obtained when an SP:TAβCD (1:1 molar ratio) spray-dried complex was used for the nano-encapsulation and SEM analysis revealed the absence of free SP crystals. The encapsulation efficiency (%EE) and drug loading (%DL) were 85% and 2.6%, respectively, as opposed to the much lower values (14% and 0.6%, respectively) achieved with pristine SP. Moreover, the NPs sustained the SP release with relatively low burst effect of 20%. Overall, our results confirmed that spray-drying of SP/TAβCD solutions at the appropriate molar ratio leads to the hydrophobization of the relatively hydrophilic SP molecule, enabling its encapsulation within mPEG-PCL NPs and paves the way for the use of this strategy in the development of novel drug delivery systems of this vital biological precursor.

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Section: Resultsmentioning

confidence: 99%

Enhanced Nanoencapsulation of Sepiapterin within PEG-PCL Nanoparticles by Complexation with Triacetyl-Beta Cyclodextrin

Kuplennik

Sosnik

2019

Molecules

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“…The entrapment efficiency was calculated according to the following equation, and each result was the mean of three determinations ±SD. 13 EE%…”

Section: Evaluation Of Cinnarizine Transfersomesmentioning

confidence: 99%

<p>Formulation and Characterization of Cinnarizine Targeted Aural Transfersomal Gel for Vertigo Treatment: A Pharmacokinetic Study on Rabbits</p>

Abdelmonem¹,

Hamed²,

Abdel-Halim³

et al. 2020

IJN

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Introduction and Aim: Cinnarizine is indicated orally for treating vertigo associated with Ménière's syndrome and has a local anesthetic effect as well. The present study aims to develop an aural Cinnarizine mucoadhesive transfersomal gel to overcome the first-pass metabolism. Methods: Eighteen Cinnarizine transfersomes were prepared by the thin-film hydration technique using different types of phosphatidylcholine and edge activators in different ratios. Formulae were tested for their appearance, entrapment efficiency, and in-vitro drug release after eight hours. F1, F4, F7, F9, F10, and F12 were selected to be examined for particle size, polydispersity index, and zeta potential. According to the previous parameters, F1 and F10 were incorporated into gels using different polymers according to factorial design 23. The eight gels were tested for appearance, pH, mucoadhesion, spreadability, drug content, in-vitro drug release after eight hours, and rheology. The transfersomal gel F1A was subjected to FTIR analysis and in-vivo pharmacokinetic study. Results: The transfersomal dispersion colors were ranging between the white and yellow. Their EE % ranged from 64.36±1.985% to 94.09±1.74%, and their in-vitro release percentages were between 61.82±1.92% and 95.92±1.18%. Also, the vesicles PS ranged from 212.3 ±30.05nm to 2150±35.35nm, DI from 0.238±0.134 to 1±0.00 and zeta potential from −57.5 ±2.54 to +4.73±1.57 mV. The transfersomal gels showed pseudoplastic behavior, pH range of 5.5 to 8, a mucoadhesive force of 169.188±1.26 to 321.212±6.94 (dyne/cm 2 ×10 2), spreadability of 40 ±7.03mm to 138 ±3.77mm, and in-vitro drug release of 81.63±1.128% to 97.78 ±0.102%. The IR spectra of the (drug-excipients) physical mixture revealed that there were no shifts of incompatibility. The in-vivo pharmacokinetic study illustrated that [AUC] 0-24 of F1A was significantly higher than that of tablets at (P< 0.05), equivalent to 703.563±26.470 and 494.256±9.621ɲg.hr/mL respectively. Conclusion: The study revealed that Cinnarizine aural mucoadhesive targeted delivery provides an improved systemic bioavailability over the conventional oral route.

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“…Zeta potential below -25 mV and above + 25mV are required for full electrostatic stabilization of the formulation. The main factor which may not show an exact result in characterization is entrapment efficiency 34 . Entrapment efficiency may affect by the concentration of lipid and surfactant.…”

Section: Characterization Of Slnmentioning

confidence: 99%

Solid lipid nanoparticles: a promising technology for delivery of poorly water-soluble drugs

Bhatt¹,

Sharma²,

Singh³

et al. 2018

actapharm

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Oral administration of drugs having low water solubility is hampered by various enzymatic barriers present in gastrointestinal (GI) tract. Lipid nanoparticles based on solid matrix have emerged as a potential drug delivery system to improve the absorption and bioavailability of several drugs, especially lipophilic compounds. Solid lipid nanoparticles (SLN) are reported as the most promising technology for oral administration and offered several advantages over conventional dosages formulations including, enhancement in solubility, stability, permeability, and bioavailability with minimal side effects. In this review, we have highlighted recent advances in the development of SLN for the oral, parenteral, rectal, and topical administration of various drugs. We have also summarized the applications of SLN in the treatment of various diseases like tuberculosis, cancer, diabetes, and several nervous system related disorders. sustained release, timed release, extended release, and targeted release of a drug. The predominance of nanoparticles over the other drug delivery systems enables them to use for drug targeting. Nanoparticles are 10-100nm in size in which drug is either dispersed or entrapped in a matrix, encapsulated as the solid solution or may be adsorbed on the surface 2 .The nanoparticles are designed to provide intimate contact with GI epithelium, prolong residence time and allow permeation across the cell membrane. A pre-systemic metabolism of a drug can be avoided by using nanoparticles 3 . Lipid nanoparticles are safe to use as they contain lipids, which are included in the category of generally recognized as safe (GRAS). Solid Lipid NanoparticlesSolid lipid nanoparticles are an advanced and rapidly budding field of nanotechnology with several applications in pharmaceutical science. SLN were developed first in 1991. These are the colloidal carriers possesses an average diameter of 10 to 1000nm. They composed of single lipid core matrix dispersed in an aqueous surfactant solution. The carriers like liposomes, polymeric micelles, and porous solids can also be used to enhance the aqueous solubility of a drug. But SLN not only helps to increase the solubility of a drug but also offers target release of drugs. SLN can be used as a carrier for lipophilic as well as hydrophilic drugs 4 . SLN provides stability to the solid lipid matrix and overcomes the disadvantages of liposomes, which includes stability problems 5 . Instead of polymeric nanoparticles, SLN are found to be more compatible with the biological system. Exclusive properties of SLN such as smaller size, larger surface area and interaction of phases at the interface make them valuable candidate 2 . The release of encapsulated compounds is controlled by solid lipid matrix, which also improves the stability of incorporated lipophilic ingredients. The type of lipids, surfactants and their concentration in the formulation of SLN adjust the particle size, drug loading, and release behavior of drugs 5 . The physicochemical characteristics of the solid lipid...

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Encapsulation challenges, the substantial issue in solid lipid nanoparticles characterization

Cited by 46 publications

References 62 publications

Enhanced Nanoencapsulation of Sepiapterin within PEG-PCL Nanoparticles by Complexation with Triacetyl-Beta Cyclodextrin

Enhanced Nanoencapsulation of Sepiapterin within PEG-PCL Nanoparticles by Complexation with Triacetyl-Beta Cyclodextrin

<p>Formulation and Characterization of Cinnarizine Targeted Aural Transfersomal Gel for Vertigo Treatment: A Pharmacokinetic Study on Rabbits</p>

Solid lipid nanoparticles: a promising technology for delivery of poorly water-soluble drugs

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