Solid lipid nanoparticles of irbesartan: preparation, characterization, optimization and pharmacokinetic studies

Soma, Deepthi; Attari, Zenab; Reddy, M. Sreenivasa; Atmakuri, Damodaram; Koteshwara, KB

doi:10.1590/s2175-97902017000115012

Cited by 50 publications

(28 citation statements)

References 13 publications

(13 reference statements)

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“…Samples after appropriate dilutions in Milli Q water were taken for analysis. 16 Particle size analysis for the formulations was carried out following proper dilutions in Milli Q water at 25.1°C with equilibration time 70 s in triplicate.…”

Section: Particle Size Analysismentioning

confidence: 99%

Effect of Surfactant on Azithromycin Dihydrate Loaded Stearic Acid Solid Lipid Nanoparticles

Bhattacharyya¹,

Reddy²

2019

tjps

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ÖZAmaç: Azitromisin dihidrat, çeşitli bakteriyel enfeksiyon tiplerinin tedavisinde kullanılan bir makrolid antibiyotiktir. Etkin madde düşük çözünürlüğü nedeniyle düşük oral biyoyararlanım gösterir. Bu çalışmada, etken maddenin çözünürlüğünü ve çözünme hızını arttırmaya yönelik olarak azitromisin dihidratın katı lipit nanopartikülleri formüle edilmiştir. Gereç ve Yöntemler: Azitromisin dihidrat yüklü stearik asit nanopartikülleri, etken madde miktarını sabit tutarken, farklı lipit yüzey aktif madde oranında üç farklı yüzey aktif madde, Tween 20, Poloksamer 188 ve Poloksamer 407 kullanılarak yüksek hızlı homojenizasyon yöntemi ile formüle edilmiştir. Bu yöntemle on iki formülasyon hazırlanmıştır. Elde edilen nanopartiküller etken madde içeriği, % etken madde yükleme, % enkapsülasyon etkinliği, partikül boyutu analizi, zeta potansiyeli, yüzey morfolojisi, Fourier Transmisyon kızılötesi spektroskopisi, in vitro etken madde salımı, stabilite çalışması için değerlendirilmiştir. Bulgular: Tüm formülasyonlar, iyi yükleme etkinliği ve lenfatik absorpsiyon için uygun bir partikül büyüklüğü ile yüksek oranda in vitro salım göstermiştir. Poloksamer 188 ile formüle edilen nanopartiküller, diğer sürfaktanlara kıyasla daha iyi özellikler göstermiştir. Sonuç: Bu çalışma, yüksek hızlı homojenizasyon yöntemiyle hazırlanan azitromisin dihidratın stearik asit nanopartiküllerinin, çözünmenin ve dolayısıyla ilacın oral biyoyararlanımının iyileştirilmesi için kullanılabileceğini göstermiştir. Anahtar kelimeler: Azitromisin dihidrat, katı lipit nanopartiküller, zeta potansiyeli, partikül büyüklüğü, enkapsülasyon verimi, ilaç salımı Objectives: Azithromycin dihydrate is a macrolide antibiotic used for the treatment of several types of bacterial infections. The drug shows low oral bioavailability due to its low solubility. In the present work solid lipid nanoparticles of azithromycin dihydrate were formulated, keeping in view enhancement of the solubility and rate of dissolution of the drug. Materials and Methods: Azithromycin dihydrate loaded stearic acid nanoparticles were formulated by high shear homogenization using three different surfactants, namely Tween 20, poloxamer 188, and poloxamer 407, at a varied lipid surfactant ratio while keeping the quantities of the active ingredient constant. Twelve such formulations were prepared. The nanoparticles obtained were evaluated for drug content, % drug loading, % entrapment efficiency, particle size analysis, zeta potential, surface morphology, Fourier transmission infrared spectroscopy, in vitro drug release, and stability. Results: All the formulations showed good entrapment efficiency and high percentage of in vitro release with a particle size suitable for lymphatic absorption. The nanoparticles formulated with poloxamer 188 showed better characteristics compared to the other surfactants. Conclusion: This study indicates that stearic acid nanoparticles of azithromycin dihydrate prepared by high shear homogenization can be successively used for improvement of dissolution and thereby ora...

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Section: Particle Size Analysismentioning

confidence: 99%

Effect of Surfactant on Azithromycin Dihydrate Loaded Stearic Acid Solid Lipid Nanoparticles

Bhattacharyya¹,

Reddy²

2019

tjps

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“…Also, it was observed that increase in drug payload resulted in sustained drug release pattern ( Figure 10) [19]. Sustained release pattern could possibly delay drug clearance, resulting in higher CFX blood level [48]. Drug release data was fitted well in to different kinetic-models which revealed that release of drug followed zero order kinetics (Table 3).…”

Section: Discussionmentioning

confidence: 94%

Binary Solid Lipid Nanosuspension Containing Cefixime: Preparation, Characterization and Comparative In-vivo Evaluation

Kamran¹,

Khan²,

Rehman³

et al. 2019

Preprint

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Current study focused on resolution of poor oral bioavailability issues of cefixime through fabrication of its freeze dried binary solid lipid nano particles (SLNs). The nano formulation fabricated via hot melt encapsulation (HME) method was optimized using numerous formulation variables. Optimized nano formulation (CFX-4) showed particle size 206.6±2.3 nm, polydispersity index (PDI) 0.271±0.03, zeta potential (ZP) -30.7±3.1 mV, encapsulation efficiency (EE%) 88.2±2.3% along with drug loading capacity (DLC%) 4.83±0.16%. Micrograph of scanning electron microscopy (SEM) represented spherical shaped particles. Reduction in drug’s crystalline nature was acknowledged through differential scanning calorimetry (DSC) and x-ray powder diffraction (P-XRD) analysis. Drug-excepient compatibility was established through fourier transform infrared spectroscopic (FT-IR) analysis. During in-vitro studies; sustained drug release was favored by increased drug payload. Stability studies exposed that refrigerated temperature imparts maximum stability to binary SLNs. In-vivo pharmacokinetic studies revealed the desired enhancement in oral bioavailability compared to the marketed product (Cefiget®). Presented investigations established the dominance of binary SLNs for improvement of oral bioavailability with sustained drug release characteristics. Based on the reported outcomes, binary SLNs can be employed as an advanced drug delivery system for other hydrophobic drugs.

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“…These results are in full agreement with (Soma et al, 2013), who studied the effect of increasing GMS on Irbesartan loaded SLNs. They proved that increasing concentration of GMS increased EE% [20].…”

Section: The Effect Of Lipid Concentration On Ee %mentioning

confidence: 96%

“…Infrared spectra of physical mixtures of pure TFH with each one of the used excipients, namely GMS, Tween 80 and Cremophor40, as well as those of the selected optimum formulae, were investigated using KBr discs. The IR spectra were obtained in the spectral region 4000-400 cm -1 [20].…”

Section: Infrared (Ir) Spectroscopymentioning

confidence: 99%

FORMULATION AND OPTIMIZATION OF TERBINAFINE HCl SOLID LIPID NANOPARTICLES FOR TOPICAL ANTIFUNGAL ACTIVITY

Abobakr

Fayez

Elwazzan

et al. 2019

Int J Pharm Pharm Sci

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Objective: Solid lipid nanoparticles (SLNs) are at the forefront of the rapidly developing field of nanotechnology with several potential applications in drug delivery and research. The aim of this study was to develop and characterize SLNs formulae of Terbinafine HCl (TFH) for topical drug delivery applications.Methods: SLNs were prepared using the solvent injection technique. Glyceryl Monostearate (GMS) served as the lipid base. Three stabilizers; Tween 80, Cremophor RH40, and Poloxamer 188, were used. The effect of stabilizer type and concentration, as well as the lipid concentration, were studied, factorial design of 3 2 *2 1 was applied. The prepared SLNs were characterized regarding their particle size, zeta potential, polydispersity index (PDI), entrapment efficiency percent (EE %), and physicochemical stability. The selected formulae were subjected to further investigations such as morphological studies, in vitro release studies, and Infrared (IR) spectroscopy. They were compared with the marketed cream Lamifen ® in term of their antifungal activity against Candida albicans.Results: Lipid concentration, together with the type and concentration of stabilizer, appeared to be the main cornerstones which affect the formation of SLNs. Smaller particle size was observed when increasing the stabilizer concentration and decreasing the lipid concentration. Higher EE% was observed when increasing both the stabilizer and the lipid concentrations. Formulae (F6, F12 andF19) were selected as the most suitable SLNs with optimum particle size of 480.2±18.89, 458.6±12.45 and 246.7±10.5 nm, respectively as well as the highest EE% of 87.13±0.19, 93.69±0.7 and 95.06±0.25, respectively. In vitro microbiological screening of their antifungal activity showed significantly larger zones of inhibition of diameters 25.9±0.25, 25±0.35 and 24.67±0.36 mm, respectively in comparison with the marketed Lamifen® cream which showed a zone of 11.2±0.44 mm diameter. Conclusion:Applying SLNs containing TFH as topical antifungal preparations may be considered as a very promising option as they show good physicochemical characterization with high antifungal activity, which delineates them as a promising dosage form for topical antifungal treatment.

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Solid lipid nanoparticles of irbesartan: preparation, characterization, optimization and pharmacokinetic studies

Cited by 50 publications

References 13 publications

Effect of Surfactant on Azithromycin Dihydrate Loaded Stearic Acid Solid Lipid Nanoparticles

Effect of Surfactant on Azithromycin Dihydrate Loaded Stearic Acid Solid Lipid Nanoparticles

Binary Solid Lipid Nanosuspension Containing Cefixime: Preparation, Characterization and Comparative In-vivo Evaluation

FORMULATION AND OPTIMIZATION OF TERBINAFINE HCl SOLID LIPID NANOPARTICLES FOR TOPICAL ANTIFUNGAL ACTIVITY

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