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Nanocarrier Technologies for Enhancing the Solubility and Dissolution Rate of Api
Published in Debarshi Kar Mahapatra, Sanjay Kumar Bharti, Medicinal Chemistry with Pharmaceutical Product Development, 2019
Ashwini Deshpande, Tulshidas S. Patil
These are the excipients with HLB value greater than 12 and these possess ability to self-emulsify and thus used in self-emulsifying drug delivery systems. These synthesized as a mixture of polyethylene glycols (PEG) with hydrolyzed vegetable oils. Also, the reactions of ethylene oxide with alcohol and sorbitan esters give cetostearyl alcohol ethoxylates (cetomacragol) and ether ethoxylates. Cremophor, is another class of compound widely used as a water-soluble surfactant. It includes ethoxylated hydrogenated castor oil (Cremophor RH 40 and RH 60) and non-hydrogenated castor oil, e.g., ethoxylated castor oil (Cremophor EL).
Medication: Nanoparticles for Imaging and Drug Delivery
Published in Harry F. Tibbals, Medical Nanotechnology and Nanomedicine, 2017
Paclitaxel has demonstrated effectiveness in shrinking many types of lung tumors, but some of the earlier emulsion formulations of paclitaxel caused allergic reactions. This was found to be associated with a surfactant used to make the nanoparticles (Cremophor). A Cremophor-free particle formulation of paclitaxel (Abraxane) is now available, with promising results. The nanoparticles are composed of paclitaxel bonded with albumin to minimize any source of allergic reaction [398].
Biomaterials and drug delivery systems for intraperitoneal chemotherapy
Published in Wim P. Ceelen, Edward A. Levine, Intraperitoneal Cancer Therapy, 2015
PTX is poorly water-soluble and, thus, requires a solubility enhancer. An equal parts mixture of ethanol and Cremophor EL (polyethoxylated castor oil) is used to solubilize PTX in Taxol® [78,105]. Alternative solubilization strategies are pursued to reduce toxicities related to Cremophor EL. For example, PTX and randomly methylated-β-cyclodextrin (RAME-β-CD) form water-soluble inclusion complexes, which does not precipitate upon dilution and stay stable after 24-hour storage at ambient temperature or 2 hours at 41.5°C [8]. When used for hyperthermic peritoneal perfusion, PTX/RAME-β-CD complexes showed 40-fold higher plasma concentration than Taxol in a rat model [6] and delayed the growth of peritoneal carcinomatosis [7]. The authors argued that PTX/RAME-β-CD complexes had a greater ability to penetrate into IP tumors than Taxol, which entrapped PTX in surfactant micelles and thus limited direct tumor exposure of the drug [6].
Efficacy and safety of nanoparticle albumin-bound paclitaxel in non-small cell lung cancer: a systematic review and meta-analysis
Published in Artificial Cells, Nanomedicine, and Biotechnology, 2019
Paclitaxel, extracted from the bark of the Pacific yew, plays an essential role in the treatment of advanced NSCLC [3,4]. Because of its poor aqueous solubility, the standard commercial formulation of paclitaxel consists of the cremophor EL (CrEL) solvent system and ethanol, which can provoke serious toxicities, such as nephrotoxicity, endothelial toxicity, neurotoxicity, hypersensitivity and even irreversible sensory neuropathy [5,6]. To minimize the risk of hypersensitivity reactions caused by cremophor, the administration of CrEL requires a long infusion period (typically 3–24 h), in-line filters, and premedication with steroids and antihistamines [4]. Regardless of these precautions, severe and even fatal hypersensitivity reactions still occur. Additionally, the sb-paclitaxel cremophor excipient traps paclitaxel in micelles, which results in nonlinear pharmacokinetics [7]. Therefore, we urgently need to develop additional treatment strategies with high efficiencies and less toxicities for patients with NSCLC.
Revaprazan-loaded surface-modified solid dispersion: physicochemical characterization and in vivo evaluation
Published in Pharmaceutical Development and Technology, 2019
Jong Hyuck Park, Jung Hyun Cho, Dong Shik Kim, Jung Suk Kim, Fakhar Ud Din, Jong Oh Kim, Chul Soon Yong, Yu Seok Youn, Kyung Taek Oh, Dong Wuk Kim, Han-Gon Choi
Subsequently, the influence of the amount of carriers, with a constant ratio of HPMC/Cremophor A25 (1:4), on drug solubility was evaluated (Table 2, composition VI–IX). Drug solubility was increased in the following composition order IX < VII < VI < VIII. Similarly, the drug solubility was significantly increased with up to 1.4 g carrier amounts (composition VIII), followed by an abrupt decrease at 5 g carrier amounts (composition IX). Relatively high carrier amounts, i.e. more than 5 g, might hinder the drug solubility in the SMSD (Yousaf, Kim, Kim, Chang, et al. 2015). Thus, the optimal amount of carrier should be chosen to ensure maximum drug solubility for the SMSD (Li et al. 2010; Lee et al. 2013). Composition VIII enhanced drug solubility ∼6000-fold, compared to revaprazan powder (16845.75 ± 2228.82 vs. 2.81 ± 0.73 μg/ml). The SMSD composed of revaprazan/HPMC/Cremophor A25 at the weight ratio of 1:0.28:1.12 was selected for further study. Although the amount of Cremophor A25 looks high compared with the drug, total carrier amount (1.4 g) was relatively lower than general solid dispersion systems.
Cardiotoxicity of cancer chemotherapy in clinical practice
Published in Hospital Practice, 2019
Taxanes (paclitaxel and docitaxel) are a class of diterpenes that are used for treating breast, lung, pancreatic, bladder, prostatic and ovarian cancers, and Kaposi’s sarcoma [51–55]. Paclitaxel was originally identified from the bark and needles of the plants in Taxus genus (Pacific yews). Docitaxel is a derivative of paclitaxel. These agents act by disrupting the microtubular function in the cells by acting on protein tubulin. Microtubules are essential for cell division. Therefore these agents are mitosis inhibitors. Paclitaxel is highly insoluble in water, and Cremophor EL (polyethoxylated castor oil) is used as a solvent [53]. Cremophor EL is also used as a solvent for several other water-insoluble or poorly soluble pharmaceutical agents. Cremophor EL is not biological inert and results in several adverse biological effects. Some of the side effects observed with paclitaxel such as chest tightness, shortness of breath, peripheral neuropathy, sinus bradycardia, and anaphylactic reactions are related to this solvent. Albumin bound nanoparticle paclitaxel (Abraxane™) avoids the toxicity associated with the solvent Cremophor EL [54,55].