Formulation Development and Evaluation of Solid Lipid Nanoparticles of Aceclofenac Using Solvent Injection Method.

Amaç: Son 20 yılda nanoteknolojik gelişmeler ile birlikte ilaç moleküllerinin beyne hedeflenmesine yönelik çalışmalarda artış gözlenmektedir. Beyin, kan dolaşımından kendine özgü bir bariyer ile ayrılmıştır. Kan-beyin bariyeri olarak adlandırılan bu yapı astrosit, perisit, endotel hücreleri ve bunlar arasında bulunan sıkı bağlantılardan oluşmaktadır. Moleküllerin beyne geçişini engelleyen enzimatik aktivitenin yanında, beynin sistemik dolaşımdan kan-beyin bariyeri ile ayrılması, terapötik moleküllerinin beyne geçişini olumsuz etkilemektedir. Bu yüzden merkezi sinir sistemi rahatsızlıklarında tedavi zorlaşmakta, terapötik etki azalmakta veya gözlenememektedir. Bu durumu anlamak ve olası sorunları giderebilmek için beynin ve kan-beyin bariyerinin yapısı bilinmeli, ilaç moleküllerinin geçiş mekanizmaları aydınlatılmalıdır. Beyne hedeflemede ilaç taşıyıcı sistemlerin önemi günden güne artmaktadır. Üretilen sistemler arasında katı lipit nanopartiküllerin kolay üretimi, biyo-uyumluluğu, biyo-bozunabilirliği açısından diğer sistemlere göre avantajları bulunmaktadır. Bu derlemede, kan beyin bariyerinden bahsedilmesi, beyne ilaç hedefleme yöntemlerinin açıklanması ve beyne ilaç moleküllerinin hedeflenmesinde katı lipit nanopartiküllerle yapılan çalışmalardan söz edilmesi amaçlanmıştır.Sonuç ve Tartışma: İlaç moleküllerinin beyne hedeflenmesinde kan-beyin bariyeri en büyük engeldir. Bu engeli aşabilmek amacıyla geliştirilen sistemlerden biri de katı lipit nanopartiküller olmuş, sayısız çalışmalarla etkinliği kanıtlanmıştır. Hedefleme ile merkezi sinir sistemi rahatsızlıklarında ilaçların etkinliğinin arttırılabileceği görülmüştür.

show abstract

“…Bir iğne yardımı ile su fazına damla damla eklenir. Lipit damlalar katılaşır ve nano boyutta tanecikler elde edilir [39].…”

Section: çöZücü Enjeksiyon Yöntemiunclassified

Kati Li̇pi̇t Nanoparti̇küller Ve Beyne Özgü İlaç Taşiyici Si̇stem Olarak Uygulamalari

Toksoy¹,

Tirnaksiz²

2021

Ankara Universitesi Eczacilik Fakultesi Dergisi

View full text Add to dashboard Cite

show abstract

“…Based on the viscosity of medium the DLS intensity was ixed by the instrument itself, i.e., for high viscous sample the instrument will ix 170º light scattering intensity and for low viscous samples the instrument will ix 90º light scattering intensity. All quanti ication were done in triplicate (n=3) and the inal outcome should obey the ideal characteristics of a NLC Particle size: 10-1000 nm PI should be : less than 0.3 [19][20][21][22][23][24][25][26][27][28][29][30] .…”

Section: Evaluation Proceduresmentioning

confidence: 99%

“…The prepared NLC was diluted and were injected into the probe in an electrophoretic cell through which an electric ield (80 mV) was supplied [76]. All quanti ications were carried out in triplicate at 25 • C. By using the Smolochowski equation, the Zeta potential of NLC was determined directly [19][20][21][22][23][24][25][26][27][28][29][30] . N3 formulation of Lovastatin was selected as the optimized formulation.…”

Section: Zeta Potential (ζ)mentioning

confidence: 99%

See 1 more Smart Citation

Design, optimization and invitro evaluation of lovastatin nanostructures lipid carrier

Pawar¹,

Kalaiselvan²,

Balamurugan³

2020

ijprls

View full text Add to dashboard Cite

The intention of this current study is to intensify the bioavailability of drugs which have lower bioavailability (<20 %) like Lovastatin in the form of NLC carrier and also to optimize the formulation to select perfect variables for the formulation. The Nanostructures lipid carrier was formulated using Hot Homogenization technique with some optimization by utilizing 23 factorial design with the heal of response like in-vitro drug release, % Entrapment Efϑiciency (EE%), % drug Content (%DC), Zeta potential (Zp), Polydispersity Index (PI) and Particle Size (PS) for 12 hours. The kinetic studies of in-vitro drug release was performed and the parameters of the drug in different kinetic models like higuchi kinetic, zero order, ϑirst order, peppas models were evaluated. Invitro release kinetics studies show that optimized formulation NLC (N3) obeys Super Case II kinetics transport mechanism i.e., release of drug through reduction of attractive forces between Lipid chains and Zero order release kinetics for controlled drug delivery. Hence Nanostructure lipid carrier shows a good control and predetermined rate of drug release of Lovastatin. From the obtained outcome, N3 formulation was concluded as an optimized formulation with selected formulation variables like Solid Lipid: Liquid Lipid ratio (6:4), Span 80 as Surfactant (1%) and process variables like homogenization Speed as 5000 Rotations per minute for 15 mins.><20 %) like Lovastatin in the form of NLC carrier and also to optimize the formulation to select perfect variables for the formulation. The Nanostructures lipid carrier was formulated using Hot Homogenization technique with some optimization by utilizing 23 factorial design with the heal of response like in-vitro drug release, % Entrapment Efficiency (EE%), % drug Content (%DC), Zeta potential (Zp), Polydispersity Index (PI) and Particle Size (PS) for 12 hours. The kinetic studies of in-vitro drug release was performed and the parameters of the drug in different kinetic models like higuchi kinetic, zero order, first order, peppas models were evaluated. Invitro release kinetics studies show that optimized formulation NLC (N3) obeys Super Case II kinetics transport mechanism i.e., release of drug through reduction of attractive forces between Lipid chains and Zero order release kinetics for controlled drug delivery. Hence Nanostructure lipid carrier shows a good control and predetermined rate of drug release of Lovastatin. From the obtained outcome, N3 formulation was concluded as an optimized formulation with selected formulation variables like Solid Lipid: Liquid Lipid ratio (6:4), Span 80 as Surfactant (1%) and process variables like homogenization Speed as 5000 Rotations per minute for 15 mins.

show abstract

“…Various methods are available for the preparation SLN'S which include high pressure homogenization, high speed homogenization, micro emulsion based SLN preparation, double emulsion method, solvent emulsification/ evaporation, spray drying method, super critical fluid method and solvent injection method [1,[6][7][8]. The present investigation uses solvent injection method to prepare EVG-loaded SLNs which is based on the injection of organic phase containing drug in to continuously stirred aqueous phase containing emulsifier and surfactant [9][10][11].…”

Section: Introductionmentioning

confidence: 99%

Preparation, Characterization and Evaluation of Elvitegravir-Loaded Solid Lipid Nanoparticles for Enhanced Solubility and Dissolution Rate

Kommavarapu¹,

Maruthapillai²,

Kamaraj³

2015

Trop. J. Pharm Res

View full text Add to dashboard Cite

Purpose: To enhance the aqueous solubility and dissolution rate of elvitegravir (EVG) by formulating the drug as solid lipid nanoparticles (SLNs) using solvent injection method.Methods: EVG-loaded SLNs were prepared by solvent injection method. Four different formulations of SLN were prepared using gelucire - 44/14 as lipid core in ethanol, soya lecithin as emulsifier, and polysorbate 80 as surfactant in the aqueous phase. The SLNs were characterized for various physical properties, including particle size, zeta potential, polydispersity, release profile and entrapment efficiency.Results: The yield of SLNs was in the range 151.0 ± 2.4 to 199.1 ± 2.7 nm. Significant changes were observed in mean particle size (nm), Z - potential (mV) and polydispersity index (PDI) of the SLNs by varying the concentration of cryoprotectant. EVG – SLNs demonstrated a 800 – 1030-fold enhancement in aqueous solubility compared with plain EVG. The dissolution efficiency (DE) for SLNs was > 63 % in all cases and increased up to 83 % with increasing lipid load.Conclusion: Successful preparation and characterization of elvitegravir–loaded solid lipid nanoparticles by solvent injection method has been accomplished in this study.Keywords: Elvitegravir, Solid lipid nanoparticles, Cryoprotectant, Lipid load, Entrapment efficiency

show abstract

Formulation Development and Evaluation of Solid Lipid Nanoparticles of Aceclofenac Using Solvent Injection Method.

Cited by 4 publications

References 4 publications

Kati Li̇pi̇t Nanoparti̇küller Ve Beyne Özgü İlaç Taşiyici Si̇stem Olarak Uygulamalari

Kati Li̇pi̇t Nanoparti̇küller Ve Beyne Özgü İlaç Taşiyici Si̇stem Olarak Uygulamalari

Design, optimization and invitro evaluation of lovastatin nanostructures lipid carrier

Preparation, Characterization and Evaluation of Elvitegravir-Loaded Solid Lipid Nanoparticles for Enhanced Solubility and Dissolution Rate

Contact Info

Product

Resources

About