Journals / Turkish Journal of Pharmaceutical Sciences / 2019 / Cilt: 16 - Sayı: 2

Preparation and Biopharmaceutical Evaluation of Novel Polymeric Nanoparticles Containing Etoposide for Targeting Cancer Cells

Kanser Hücrelerini Hedefleyen Etopozit İçeren Yeni Polimerik Nanopartiküllerin Hazırlanması ve Biyofarmasötik Değerlendirmesi

Pages
132–140
Publication Date
2022-11-05
DOI
—
🏛️Bibliographic metadata and full text access for this article are provided via DergiPark.
DergiPark Record ↗
✨

AI Summary & Key Takeaways

AI Insight
⚡ TL;DR(Too Long; Didn't Read)

The average targeting efficiency of drugloaded nanoparticles was 41.88±0.030% of the injected dose in the liver, 25.66±0.320% in the spleen 13.82±0.090% in the lungs, 4.52±0.300% inthe kidney, and 4.18±0.490% in the brain.Conclusion: Etoposide loaded nanoparticles was found to be effective in sustained release.

📌 3 Key Takeaways

🎯
Objective & Hypothesis:Objectives: Polymeric nanoparticles are a promising novel drug delivery system and have advantages in cancer therapy.
📊
Key Findings & Data:The aim of the present study was to prepare and evaluate novel polymericnanoparticles containing etoposide.Materials and Methods: A 32 full factorial design was used to study the effect of Eudragit EPO and Pluronic F-68 on the characterization ofnanoparticle suspensions.
💡
Conclusion & Impact:The average targeting efficiency of drugloaded nanoparticles was 41.88±0.030% of the injected dose in the liver, 25.66±0.320% in the spleen 13.82±0.090% in the lungs, 4.52±0.300% inthe kidney, and 4.18±0.490% in the brain.Conclusion: Etoposide loaded nanoparticles was found to be effective in sustained release.
🔬Design:Modeling & Simulation
📍Scope:Comprehensive Sample
⚙️Variables:Domain Parameters

Abstract

Objectives: Polymeric nanoparticles are a promising novel drug delivery system and have advantages in cancer therapy. Etoposide is an anticanceragent that is used in the treatment of a variety of malignancies. The aim of the present study was to prepare and evaluate novel polymericnanoparticles containing etoposide.Materials and Methods: A 32 full factorial design was used to study the effect of Eudragit EPO and Pluronic F-68 on the characterization ofnanoparticle suspensions. The polymeric nanoparticles were prepared by nanoprecipitation technique. The prepared nanoparticles was evaluatedby percentage yield, drug polymer compatibility using fourier transform infrared (FTIR) spectroscopy and differential scanning calorimetric (DSC)analysis, drug content, entrapment efficiency, zeta potential, particle size, scanning electron microscopy, X-ray diffraction, in vitro drug releasestudies, kinetic modeling, stability studies, and in vivo animal studies. Response surface plots were studied, which were generated using PCPdissolution software.Results: Scanning electron microscopic studies confirmed their porous structure with a number of nanochannels. The FTIR spectra showed thestable character of etoposide in a mixture of polymers and revealed the absence of drug–polymer interactions. The DSC study revealed that thedrug was involved in complexation with nanoparticles. The average particle size of etoposide nanoparticles was in the range of 114.4 nm to 136.7nm. The zeta potential values were attained to ensure good stability of nanosuspensions. In vitro release of the drug from nanoparticles followsthe Peppas model and showed controlled release behavior for a period of 24 h. The optimized nanoparticles were subjected to stability studiesat 4°C in a refrigerator and the most suitable temperature for storage of etoposide nanoparticles found. The average targeting efficiency of drugloaded nanoparticles was 41.88±0.030% of the injected dose in the liver, 25.66±0.320% in the spleen 13.82±0.090% in the lungs, 4.52±0.300% inthe kidney, and 4.18±0.490% in the brain.Conclusion: Etoposide loaded nanoparticles was found to be effective in sustained release.

Özet

Amaç: Polimerik nanopartiküller kanser tedavisinde avantajlı ve gelecek vaad eden yeni ilaç salım sistemidir. Etopozid, çeşitli malignitelerin tedavisinde kullanılan bir antikanser ajanıdır. Bu çalışmanın amacı, etopozit içeren yeni polimerik nanopartiküllerin hazırlanması ve değerlendirilmesidir. Gereç ve Yöntemler: Eudragit EPO ve Pluronic F-68’in nanopartikül süspansiyonunun karakterizasyonu üzerindeki etkisini incelemek için 32tam faktöriyel tasarım kullanılmıştır. Polimerik nanopartiküller nano presipitasyon tekniği ile hazırlanmıştır. Hazırlanan nanopartiküller, yüzde verim, fourier dönüşümü kızılötesi (FTIR) spektroskopisi ve diferansiyel taramalı kalorimetrik (DSC) analizi kullanılarak ilaç polimer uyumluluğu, etkin madde içeriği, yükleme kapasitesi, zeta potansiyeli, partikül boyutu, taramalı elektron mikroskobu, X-ışını difraksiyon, in vitro etkin madde salımçalışmaları, kinetik modelleme, stabilite çalışmaları ve in vivo hayvan çalışması ile değerlendirilmiştir. PCP çözünme yazılımı kullanılarak oluşturulan tepki yüzey grafikleri incelenmiştir. Bulgular: Taramalı elektron mikroskopisi çalışmaları çok sayıda nano-kanal içeren gözenekli yapılarını doğrulamıştır. FTIR spektrumları, polimer karışımında etopozitin stabil olduğunu ve ilaç polimer etkileşimlerinin olmadığını ortaya çıkartmıştır. DSC çalışması, etkin maddenin komplikasyon ile nanopartiküllere yüklendiğini ortaya koymuştur. Etopozid nanopartiküllerin ortalama partikül büyüklüğünün 114.4 nm ile 136.7 nm arasında olduğu bulunmuştur. Zeta potansiyel değerlerinden elde edilen sonuç nanosüspansiyonların iyi bir stabilitede olmasını sağlamıştır. Nano-partiküllerden etkin maddenin in vitro salımı Peppas’a uyumlu olup, 24 saatlik bir süre boyunca kontrollü salım göstermiştir. Optimize edilmiş nanopartiküller, 4°C’de buzdolabında stabilite çalışmalarına tabi tutulmuş ve Etopozid nanopartiküllerinin depolanması için en uygun sıcaklık olarak bulunmuştur. Etkin madde yüklü nanopartiküllerin ortalama hedefleme etkinliği, karaciğerde enjekte edilen dozun %41.88±0.030’u, dalakta %25.66±0.320’si, akciğerlerde %13.82±0.090’ı, böbreklerde %4.52±0.300’ü ve beyinde %4.18±0.490’ı olarak bulunmuştur. Sonuç: Etopozit yüklü nanopartiküllerin sürekli salımda etkili olduğu sonucuna varılmıştır.

🔖

Cite This Article

THIYAGARAJAN, A., SARAVANABHAVAN, S., THANGARASU, V. (2022). Preparation and Biopharmaceutical Evaluation of Novel Polymeric Nanoparticles Containing Etoposide for Targeting Cancer Cells. Turkish Journal of Pharmaceutical Sciences, Cilt: 16 - Sayı: 2, 132–140. https://ajindex.com/articles/613808

📄 Full Text PDF Viewer

📄

PDF görüntüleyici hazırlanıyor...

References (18)

  1. Montecucco A, Biamonti G. Cellular response to etoposide treatment. Cancer Lett. 2007;252:9-18
  2. Ezoe S. Secondary leukemia associated with the anti-cancer agent, etoposide, a topoisomerase II inhibitor. Int J Environ Res Public Health. 2012;9:2444-2453
  3. McLeod HL, Evans WE. Clinical pharmacokinetics and pharmacodynamics of epipodophyllotoxins. Cancer Surv. 1993;17:253-268
  4. Rodman JH, Murry DJ, Madden T, Santana VM. Altered etoposide pharmacokinetics and time to engraftment in pediatric patients undergoing autologous bone marrow transplantation. J Clin Oncol. 1994;12:2390-2397
  5. Hande KR. Etoposide pharmacology. Semin Oncol. 1992;19(6 Suppl 13):3- 9
  6. Joel SP, Shah R, Slevin ML. Etoposide dosage and pharmacodynamics. Cancer Chemother Pharmacol. 1994;34(Suppl):69-75
  7. Chellampillai B, Pawar AP. Improved bioavailability of orally administered andrographolide from pH-sensitive nanoparticles. Eur J Drug Metab Pharmacokinet. 2011;35:123-129
  8. Huang KJ, Zhu CH. The production and characteristics of solid lipid nanoparticles (SLNs). Biomaterials. 2003;24:1781-1785
  9. Kaliks R, Guerra C, Giglio AD. Efficacy and toxicity of mitoxantrone and oral etoposide in the treatment of hormone refractory prostate cancer: pilot study. Einstein (Sao Paulo). 2010;8:336-338
  10. Patloll RR, Vobalaboina V. Folate-targeted etoposide-encapsulated lipid nanospheres. J Drug Target. 2008;16:269-275
  11. Patlolla RR, Vobalaboina V. Pharmacokinetics and tissue distribution of etoposide delivered in parenteral emulsion. J Pharma Sci. 2005;94:437- 445
  12. Abdelbary G, Fahmy RH. Diazepam loaded solid lipid nanoparticles: design and characterization. AAPS PharmScieTech. 2009;10:211-219
  13. Kreuter J. Nanoparticles in Colloidal Drug Delivery Systems. New York; Marcel Dekker Inc; 1994:2019-220
  14. Huynh NT, Passirani C, Saulnier P, Benoit JP. Lipid nanocapsules: A new platform for nanomedicine. Int J Pharm. 2009;379:201-209
  15. Xing J, Zhan, D, Tan T. Studies on the oridonin-loaded poly(D,L-lactic acid) nanoparticles in vitro and in vivo. Int J Biol Macromol. 2007;40:153- 158
  16. Lee ES, Oh YT, Youn YS, Nam M, Park B, Yun J, Kim JH, Song HT, Oh KT. Binary mixing of micelles using pluronics for a nano-sized drug delivery system. Colloids Surf B Biointerfaces. 2011;82:190-195
  17. Kocbek P, Baumgartner S, Kristl J. Preparation and evaluation of nanosuspensions for enhancing the dissolution of poorly soluble drugs. Int J Pharm. 2006;312:179-186
  18. Ubrich N, Schmidt C, B