Tissue Distribution of Antitumor Drugs Associated with Polyalkylcyanoacrylate Nanoparticles

Couvreur, Patrick; Kanté, Boubacar; Lenaerts, Vincent; Scailteur, V.; Roland, M; Speiser, P

doi:10.1002/jps.2600690222

Cited by 144 publications

(57 citation statements)

References 15 publications

(2 reference statements)

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“…Nanoparticles provide controlled release of entrapped drugs and during this action offer protection to the drug particle against body conditions maintaining the bioactivity of the compound. Nanoparticles can be used to localize drugs in the liver, spleen and lungs since they are readily taken up by the macrophage system (11)(12)(13)(14)(15). Tailored coatings over nanoparticles help overcome reticulo-endothelial uptake of nanoparticles and thus deliver the drug across various body barriers like BBB (16).…”

mentioning

confidence: 99%

Cyclodextrin based nanosponges for pharmaceutical use: A review

Tejashri¹,

Amrita²,

Darshana³

2013

Acta Pharmaceutica

179

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Nanosponges are a novel class of hyper-crosslinked polymer based colloidal structures consisting of solid nanoparticles with colloidal sizes and nanosized cavities. Well--known examples of nanosponges are titanium-based nanosponges (1), silicon nano- Nanosponges are a novel class of hyper-crosslinked polymer based colloidal structures consisting of solid nanoparticles with colloidal sizes and nanosized cavities. These nano-sized colloidal carriers have been recently developed and proposed for drug delivery, since their use can solubilize poorly water-soluble drugs and provide prolonged release as well as improve a drug's bioavailability by modifying the pharmacokinetic parameters of actives. Development of nanosponges as drug delivery systems, with special reference to cyclodextrin based nanosponges, is presented in this article. In the current review, attempts have been made to illustrate the features of cyclodextrin based nanosponges and their applications in pharmaceutical formulations. Special emphasis has been placed on discussing the methods of preparation, characterization techniques and applications of these novel drug delivery carriers for therapeutic purposes. Nanosponges can be referred to as solid porous particles having a capacity to load drugs and other actives into their nanocavity; they can be formulated as oral, parenteral, topical or inhalation dosage forms. Nanosponges offer high drug loading compared to other nanocarriers and are thus suitable for solving issues related to stability, solubility and delayed release of actives. Controlled release of the loaded actives and solubility enhancement of poorly water-soluble drugs are major advantages of nanosponge drug delivery systems.

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mentioning

confidence: 99%

Cyclodextrin based nanosponges for pharmaceutical use: A review

Tejashri¹,

Amrita²,

Darshana³

2013

Acta Pharmaceutica

179

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“…This feature can largely improve the selectivity of the drug in tumor tissue. Generally, the blood vessels in tumor tissues have large gaps (100-800 nm) between adjacent endothelial cells, and the capillary permeability of the endothelium in newly vascularized tumors are signi-ficantly wider than those of normal organs (27)(28)(29). Due to the defective vascular architecture and poor lymphatic drainage, nanoparticles can extravasate through these gaps into extravascular spaces and accumulate inside tumor tissues (26,27).…”

Section: Discussionmentioning

confidence: 99%

“…Due to the defective vascular architecture and poor lymphatic drainage, nanoparticles can extravasate through these gaps into extravascular spaces and accumulate inside tumor tissues (26,27). This phenomenon is known as the enhanced permeability and retention (EPR) effect (28,30), which has been generally observed in many types of solid tumors. Since the prepared MPEG-PCL is small enough (~20 nm), it can increase the selectivity of the available cytotoxic agents by delivering them specifically to tumor tissue, which allows maximal accumulation and the deepest penetration into tumors.…”

Section: Discussionmentioning

confidence: 99%

Antitumor activity of monomethoxy poly(ethylene glycol)-poly (ε-caprolactone) micelle-encapsulated doxorubicin against mouse melanoma

Qian¹

2011

Oncol Rep

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Abstract. Doxorubicin (Dox) is one of the most commonly used and highly effective antineoplastic agents, but the clinical application of this broad spectrum drug is largely hampered by its poor stability and serious toxicity to normal tissues. Hence, it is essential to improve the therapeutic effect and decrease the systematic toxicity for the administration of doxorubicin. In our study, doxorubicin was incorporated into monomethoxy poly(ethylene glycol)-poly(Â-caprolactone) (MPEG-PCL) micelle by a self-assembly method. The cytotoxicity and cellular uptake efficiency of Dox-loaded MPEG-PCL (Dox/MPEG-PCL) micelle against B16-F10 murine melanoma cells was examined by the methylthiazoltetrazolium (MTT) test and flow cytometry. The antitumor activity of Dox/MPEG-PCL was evaluated in C57BL/6 mice injected subcutaneously with B16-F10 cells. Toxicity was evaluated in tumor-free mice. Meanwhile, tumor proliferation, intratumoal angiogenesis and apoptotic cells were evaluated by PCNA, CD31 staining and TUNEL assay, respectively. Encapsulation of doxorubicin in MPEG-PCL micelle improved the cytotoxicity of doxorubicin and enhanced its cellular uptake on B16-F10 cell in vitro. Administration of Dox/MPEG-PCL micelle resulted in significant inhibition (75% maximum inhibition relative to controls) in the growth of B16-F10 tumor xenografts and prolonged the survival of the treated mice (P<0.05). These anti-tumor responses were associated with marked increase of tumor apoptosis and notable reduction of cell proliferation and intratumoral microvessel density (P<0.05). The system toxicity also decreased in the Dox/MPEG-PCL group compared with free doxorubicin group. Our data indicate that the encapsulation of doxorubicin in MPEG-PCL micelle improved the anti-tumor activity in vivo without conspicuous systemic toxic effects.

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“…Hasil pengukuran zeta potensial menunjukkan nanopartikel kitosanthymoquinone mempunyai zeta potensial rata-rata 137,9 mV dengan satu kali pengukuran Zeta potensial menggambarkan potensial elektrik dari partikel dan medium tempat partikel tersebut terdispersi. Nanopartikel yang memilki zeta potensial diatas ± 40 mV menunjukkan suspensi yang stabil, hal ini dikarenakan muatan permukaan akan mencegah agregasi antar partikel (Avadi et al, 2010).Zeta potensial juga dapat digunakan untuk menentukan apakah muatan zat aktif telah terenkapsulasi didalam nanocapsule atau teradsorbsi ke dalam permukaan (Couvreur et al, 2002). Dari hasil pengukuran besarnya zata potensial yaitu 137,9 mV.…”

Section: Gambarunclassified

Pengembangan Preparasi Nanopartikel Thymoquinone-Kitosan Dengan Metode Kosolven Menggunakan Isopropil Alkohol

Binarjo

Yuwono²,

Priyanti³

2015

Pharmaciana

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ABSTRAKThymoquinone, hasil isolasi dari biji jintan hitam (Nigella sativa L.) terbukti memiliki khasiat sebagai antikanker, antiinflamasi, dan immunodilator. Thymoquinone mudah menguap, mudah teroksidasi, titik lebur rendah, menyebabkan sulit diformulasi menjadi sediaan padat. Sifatnya yang tidak larut dalam air menyebabkan bioavaibilitasnya rendah. Untuk mengatasi dua masalah tersebut dilakukan pengembangan sistem penghantaran obat nanopartikel . Nanopartikel kitosan-thymoquinone dapat dibentuk dengan cross-linker natrium tripolifosfat dengan metode kosolven. Larutan thymoquinone dalam 75%, 50%, 100% isopropil alcohol dicampur dengan larutan kitosan dalam dapar asetat pH 4. Larutan Na-TPP dalam air ditambahkan sedikit demi sedikit dengan pengadukan pelan. Dilakukan karakterisasi terhadap nanopartikel meliputi loading capacity (LC), bentuk partikel, ukuran partikel, dan zeta potensial, dan karakterisasi proses preparasi yaitu nilai loading efficiency (LE). Optimasi Factorial Design menghasilkan kondisi terbaik yaitu dengan solven isopropil alkohol 75%, kadar thymoquinone 10 mg/mL,dan kadar kitosan 10 mg/mL menghasilkan nanopartikel dengan LC 8,71%, LE 76,29%, diameter rata-rata 609,8 nm dan zeta potensial rata-rata 137, 9 mV, bentuk bulat. Isopropil alcohol dapat membantu pembentukan nanopartikel thymoquinone. Ukuran partikel dan zeta potensial yang dihasilkan besar, oleh karena itu diperlukan modifikasi kadar thymoquinone, kitosan, dan Na-TPP.Keywords : Nanopartikel, thymoquinone, isopropil alkohol, polimer kitosan ABSTRACT Thymoquinone, an active compound isolated from black cumin seeds (Nigella sativa L.), has pharmacological activity as anticancer, antiinflammatory, and immunomodulator. This compound has a volatile nature, easily oxidized, and low melting point, leading to difficulties in tablet formulation. Moreover, its low solubility in water leading to low bioavailability. Therefore, it is necessary to develop nanoparticle drug delivery systems to solve these problems. Chitosan-thymoquinone nanoparticles can be formed using sodium tripolyphosphate as cross linker by cosolven method. Chitosan solution in acetate buffer pH 4 was added to thymoquinone solution in 50%, 75%, 100% isopropyl alcohol, than sodium tripoliphosphate solution in water was added slowly in a gently stirrer. The nanoparticle produced was characterized in its loading capacity (LC), particle morphology, particle size, and zeta potential, as well as the loading efficiency (LE) of nanoparticle. Factorial Design Optimization resulted that the best condistion is achieved by 75% isopropyl alcohol using thymoquinone level of 10 mg/mL and chitosan level of 10 mg/mL. In this condition, the nanoparticle has LC of 8.71%, LE of 76.29%, 609.8 nm in diameter and zeta potential of 137.9 mV. It can be concluded that isopropyl alcohol can help the formation of nanoparticles thymoquinone. The particle

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Tissue Distribution of Antitumor Drugs Associated with Polyalkylcyanoacrylate Nanoparticles

Cited by 144 publications

References 15 publications

Cyclodextrin based nanosponges for pharmaceutical use: A review

Cyclodextrin based nanosponges for pharmaceutical use: A review

Antitumor activity of monomethoxy poly(ethylene glycol)-poly (ε-caprolactone) micelle-encapsulated doxorubicin against mouse melanoma

Pengembangan Preparasi Nanopartikel Thymoquinone-Kitosan Dengan Metode Kosolven Menggunakan Isopropil Alkohol

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