Duloxetine HCl Lipid Nanoparticles: Preparation, Characterization, and Dosage Form Design

Patel, Ketan; Padhye, S G; Nagarsenker, Mangal S.

doi:10.1208/s12249-011-9727-6

Cited by 67 publications

(30 citation statements)

References 22 publications

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“…showed moderate solubility of LF (Table 2). The higher solubility in rice germ oil may be attributed to its high oleic acid content and γ-orizynol [9]. Oleic acid showed significantly higher solubility of lumefantrine – 157 mg of LF/gm of oleic acid.…”

Section: Resultsmentioning

confidence: 99%

Design and evaluation of Lumefantrine – Oleic acid self nanoemulsifying ionic complex for enhanced dissolution

2013

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BackgroundLumefantrine, an antimalarial molecule has very low and variable bioavailability owing to its extremely poor solubility in water. It is recommended to be taken with milk to enhance its solubility and bioavailability. The aim of present study was to develop a Self Nanoemulsifying Delivery system (SNEDs) of lumefantrine (LF) to achieve rapid and complete dissolution independent of food-fat and surfactant in dissolution media.MethodsSolubility of LF in oil, co-solvent/co-surfactant and surfactant solution and emulsification efficiency of surfactant were analyzed to optimize the LF loaded self nanoemulsifying preconcentrate. Effect of LF-oleic acid complexation on emulsification, droplet size, zeta potential and dissolution were investigated. Effect of milk concentration and fat content on saturation solubility and dissolution of LF was investigated. Dissolution of marketed formulation and LF-SNEDs was carried out in pH 1.2 and pH 6.8 phosphate buffer.ResultsLF exhibited very high solubility in oleic acid owing to complexation between tertiary amine of LF and carboxyl group of oleic acid (OA). Cremophore EL and medium chain monoglyceride were selected surfactant and co-surfactant, respectively. Significantly smaller droplet size (37 nm), shift in zeta potential from negative to positive value, very high drug loading in lipid based system (> 10%), no precipitation after dissolution are the major distinguish characteristics contributed by LF-OA complex in the SNED system. Saturation solubility and dissolution study in milk containing media pointed the significant increment in solubility of LF in the presence of milk-food fat. LF-SNEDs showed > 90% LF release within 30 min in pH 1.2 while marketed tablet showed almost 0% drug release.ConclusionSelf nanoemulsification promoting ionic complexation between basic drug and oleic acid hold great promise in enhancing solubility of hydrophobic drugs.

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Section: Resultsmentioning

confidence: 99%

Design and evaluation of Lumefantrine – Oleic acid self nanoemulsifying ionic complex for enhanced dissolution

2013

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“…SLN have been successfully implemented in a wide range of applications. In the biomedical field, for instance, it has been used to increase both the solubility of several poorly soluble (Patel et al, 2012;Padhye and Nagarsenker, 2013) just to mention some. In the cosmetic industry, they have been used to encapsulate UV blockers such as 3,4,5-trimethoxybenzoylchitin (TMBC), 2-hydroxy-4-methoxybenzophenone and vitamin E for use as sunscreen (Wissing and Müller, 2001;Song and Liu, 2005).…”

Section: Solid Lipid Nanoparticles (Sln)mentioning

confidence: 99%

Nanoscale Drug Delivery Systems: From Medicine to Agriculture

Vega-Vásquez

Mosier

Irudayaraj

2020

Front. Bioeng. Biotechnol.

198

107

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The main challenges in drug delivery systems are to protect, transport and release biologically active compounds at the right time in a safe and reproducible manner, usually at a specific target site. In the past, drug nano-carriers have contributed to the development of precision medicine and to a lesser extent have focused on its inroads in agriculture. The concept of engineered nano-carriers may be a promising route to address confounding challenges in agriculture that could perhaps lead to an increase in crop production while reducing the environmental impact associated with crop protection and food production. The main objective of this review is to contrast the advantages and disadvantages of different types of nanoparticles and nano-carriers currently used in the biomedical field along with their fabrication methods to discuss the potential use of these technologies at a larger scale in agriculture. Here we explain what is the problem that nano-delivery systems intent to solve as a technological platform and describe the benefits this technology has brought to medicine. Also here we highlight the potential drawbacks that this technology may face during its translation to agricultural applications, based on the lessons learned so far from its use for biomedical purposes. We discuss not only the characteristics of an ideal nano-delivery system, but also the potential constraints regarding the fabrication including technical, environmental, and legal aspects. A key motivation is to evaluate the potential use of these systems in agriculture, especially in the area of plant breeding, growth promotion, disease control, and post-harvest quality control. Further, we highlight the importance of a rational design of nano-carriers and identify current research gaps to enable scale-up relevant to applications in the treatment of plant diseases, controlled release of fertilizers, and plant breeding.

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“…Improved bioavailability, safety, and protection against degradation of the drug payload in the stomach are some of the desirable attributes associated with oral delivery of SLNs. Furthermore, it is possible to tailor formulations to ensure controlled release of the payload from the SLNs (6)(7)(8)(9)(10). Uptake of intact SLNs via the lymphatic route into blood has been reported in some studies after oral and duodenal administrations of SLNs to rats.…”

Section: Introductionmentioning

confidence: 99%

Effect of Food Status on the Gastrointestinal Transit of Amphotericin B-Containing Solid Lipid Nanoparticles in Rats

et al. 2015

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Abstract. Amphotericin B (AmB) is poorly absorbed from the gastrointestinal tract. Recent studies have suggested enhanced drug absorption from solid lipid nanoparticles (SLN). Little is known of the fate of AmB absorption within the gastrointestinal tract, and no gastrointestinal transit study has yet been performed on AmB-containing nano-formulations. We aimed to investigate the effect of food on the gastrointestinal transit properties of an AmB-containing SLN in rats. Three SLNs containing AmB, paracetamol, or sulfasalazine were formulated using cocoa butter and beeswax as lipid matrices and simultaneously administered orally to Sprague-Dawley rats. Paracetamol and sulfapyridine were used as marker drugs for estimating gastric emptying and cecal arrival, respectively. The pharmacokinetic data generated for paracetamol and sulfapyridine were used in estimating the absorption of the AmB SLNs in the small and large intestines, respectively. A delayed rate of AmB absorption was observed in the fed state; however, the extent of absorption was not affected by food. Specifically, the percentages of AmB absorption during the fasted state in the stomach, small intestine, and colon were not significantly different from absorption within the respective regions in the fed state. In both states, however, absorption was highest in the colon and appeared to be a combination of absorption from the small intestine plus absorption proper within the colon. The study suggests that AmB SLN, irrespective of food status, is slowly but predominantly taken up by the lymph, making the small intestine the most favorable site for the delivery of the AmB SLNs.

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Duloxetine HCl Lipid Nanoparticles: Preparation, Characterization, and Dosage Form Design

Cited by 67 publications

References 22 publications

Design and evaluation of Lumefantrine – Oleic acid self nanoemulsifying ionic complex for enhanced dissolution

Design and evaluation of Lumefantrine – Oleic acid self nanoemulsifying ionic complex for enhanced dissolution

Nanoscale Drug Delivery Systems: From Medicine to Agriculture

Effect of Food Status on the Gastrointestinal Transit of Amphotericin B-Containing Solid Lipid Nanoparticles in Rats

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