Nanonized itraconazole powders for extemporary oral suspensions: Role of formulation components studied by a mixture design

Bonda, Andrea Foglio; Rinaldi, Maurizio; Segale, Lorena; Palugan, Luca; Cerea, Matteo; Vecchio, C; Pattarino, Franco

doi:10.1016/j.ejps.2015.12.030

Cited by 16 publications

(9 citation statements)

References 28 publications

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“…~73% of the formulations in Table 2 used surfactants alone or in combination with other dispersants ( Figure 8 a). Being surface-active agents, surfactants reduce the surface tension of suspension liquids, help to disperse drug particles in suspension liquid by enhancing drug wettability, and help to stabilize drug nanosuspensions either alone or in combination with polymers [ 23 , 28 , 55 , 163 ]. They also impart wettability enhancement to the nanocomposites which help to speed up redispersion and drug nanoparticle recovery [ 78 , 86 ].…”

Section: Preparation Characterization and Formulation Of Drug-lamentioning

confidence: 99%

Bioavailability Enhancement of Poorly Water-Soluble Drugs via Nanocomposites: Formulation–Processing Aspects and Challenges

et al. 2018

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Drug nanoparticles embedded in a dispersant matrix as a secondary phase, i.e., drug-laden nanocomposites, offer a versatile delivery platform for enhancing the dissolution rate and bioavailability of poorly water-soluble drugs. Drug nanoparticles are prepared by top-down, bottom-up, or combinative approaches in the form of nanosuspensions, which are subsequently dried to prepare drug-laden nanocomposites. In this comprehensive review paper, the term “nanocomposites” is used in a broad context to cover drug nanoparticle-laden intermediate products in the form of powders, cakes, and extrudates, which can be incorporated into final oral solid dosages via standard pharmaceutical unit operations, as well as drug nanoparticle-laden strip films. The objective of this paper is to review studies from 2012–2017 in the field of drug-laden nanocomposites. After a brief overview of the various approaches used for preparing drug nanoparticles, the review covers drying processes and dispersant formulations used for the production of drug-laden nanocomposites, as well as various characterization methods including quiescent and agitated redispersion tests. Traditional dispersants such as soluble polymers, surfactants, other water-soluble dispersants, and water-insoluble dispersants, as well as novel dispersants such as wet-milled superdisintegrants, are covered. They exhibit various functionalities such as drug nanoparticle stabilization, mitigation of aggregation, formation of nanocomposite matrix–film, wettability enhancement, and matrix erosion/disintegration. Major challenges such as nanoparticle aggregation and poor redispersibility that cause inferior dissolution performance of the drug-laden nanocomposites are highlighted. Literature data are analyzed in terms of usage frequency of various drying processes and dispersant classes. We provide some engineering considerations in comparing drying processes, which could account for some of the diverging trends in academia vs. industrial practice. Overall, this review provides rationale and guidance for drying process selection and robust nanocomposite formulation development, with insights into the roles of various classes of dispersants.

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Section: Preparation Characterization and Formulation Of Drug-lamentioning

confidence: 99%

Bioavailability Enhancement of Poorly Water-Soluble Drugs via Nanocomposites: Formulation–Processing Aspects and Challenges

et al. 2018

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“…Then, the virtual cocrystal screening was performed for four drugs, namely Iloperidone, Ritonavir, Carbamazepine, Ethenzamide. All these compounds belonging to the II class of Biopharmaceutics Classification System (high permeability and low solubility) have been extensively studied in terms of bioavailability and dissolution profile improvement (Aitipamula et al, 2012;Danjo, K., Nataka, T. & Otsuka, 1997;Foglio Bonda et al, 2016;Gadade et al, 2017;Ibrahim et al, 2010;Ige et al, 2015;Jitkar et al, 2016;Kojo et al, 2017;Miwa et al, 2016;Remenar et al, 2003;Six et al, 2004;Thiry et al, 2017aThiry et al, , 2016. It is understandable that not all pharmaceutically accepted excipients are miscible in the solid phase with a particular API in the form of a cocrystal.…”

Section: Resultsmentioning

confidence: 99%

Selection of effective cocrystals former for dissolution rate improvement of active pharmaceutical ingredients based on lipoaffinity index

Cysewski

Przybyłek

2017

European Journal of Pharmaceutical Sciences

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New theoretical screening procedure was proposed for appropriate selection of potential cocrystal formers possessing the ability of enhancing dissolution rates of drugs. The procedure relies on the training set comprising 102 positive and 17 negative cases of cocrystals found in the literature. Despite the fact that the only available data were of qualitative character, performed statistical analysis using binary classification allowed to formulate quantitative criterions. Among considered 3679 molecular descriptors the relative value of lipoaffinity index, expressed as the difference between values calculated for active compound and excipient, has been found as the most appropriate measure suited for discrimination of positive and negative cases. Assuming 5% precision, the applied classification criterion led to inclusion of 70% positive cases in the final prediction. Since lipoaffinity index is a molecular descriptor computed using only 2D information about a chemical structure, its estimation is straightforward and computationally inexpensive. The inclusion of an additional criterion quantifying the cocrystallization probability leads to the following conjunction criterions H<-0.18 and ΔLA>3.61, allowing for identification of dissolution rate enhancers. The screening procedure was applied for finding the most promising coformers of such drugs as Iloperidone, Ritonavir, Carbamazepine and Enthenzamide.

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“…Used to improve solubility of poorly soluble drugs [142]; medicated chewing gums [120]; bioactive dressings [128]; or tablets [121,139], oleogels [144,145], organogels for cardiovascular diseases [118], nanoparticles with amoxicillin trihydrate and thymol [131,134], novel excipients [129,136,146] and oils mixture with salicylic acid for ointment [143] formulation; itraconazole for oral [27,127], gel with loratadine [148], tablets of metformin [130], controlled release of ketoprofen [23] and excipients with finasteride [126] formulation; emulsion formulation of vitamins [119], of aceclofenac [122], of raloxifen [135], of aprepitant [123], of catechin [28], of darunavir [117], of lopinavir [116], of butenafine hydrochloride [132], of cathepsin K inhibitor [140], of telmisartan [138], of olmesartan medoxomil [137], of bovine serum albumin [141], of nelfinavir mesylate [124], of docetaxel [125], of nutraceutical products [147] and oxidative stability avocado oil [133].…”

Section: Application Of Mixture Design In Pharmaceutical Healthmentioning

confidence: 99%

“…Thus, MDs can facilitate the development of novel products or techniques that seek to achieve these goals. Among some typical applications, we can list the development of foods and beverages with functional or nutraceutical properties [22,[24][25][26], while in the pharmaceutical health area, they are used to formulate drugs for several diseases [23,27,28]. In addition, MDs can also be used for many other applications [5,29,30].…”

Section: Introductionmentioning

confidence: 99%

Recent Applications of Mixture Designs in Beverages, Foods, and Pharmaceutical Health: A Systematic Review and Meta-Analysis

Galvan

Effting

Cremasco

et al. 2021

Foods

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Design of Experiments (DoE) is a statistical tool used to plan and optimize experiments and is seen as a quality technology to achieve products excellence. Among the experimental designs (EDs), the mixture designs (MDs) stand out, being widely applied to improve conditions for processing, developing, or formulating novel products. This review aims to provide useful updated information on the capacity and diversity of MDs applications for the industry and scientific community in the areas of food, beverage, and pharmaceutical health. Recent works were selected following the Preferred Reporting Items for Systematic Review and Meta-Analyses statement (PRISMA) flow diagram. Data analysis was performed by self-organizing map (SOM) to check and understand which fields of application/countries/continents are using MDs. Overall, the SOM indicated that Brazil presented the largest number of works using MDs. Among the continents, America and Asia showed a predominance in applications with the same amount of work. Comparing the MDs application areas, the analysis indicated that works are prevalent in food and beverage science in the American continent, while in Asia, health science prevails. MDs were more used to develop functional/nutraceutical products and the formulation of drugs for several diseases. However, we briefly describe some promising research fields in that MDs can still be employed.

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Nanonized itraconazole powders for extemporary oral suspensions: Role of formulation components studied by a mixture design

Cited by 16 publications

References 28 publications

Bioavailability Enhancement of Poorly Water-Soluble Drugs via Nanocomposites: Formulation–Processing Aspects and Challenges

Bioavailability Enhancement of Poorly Water-Soluble Drugs via Nanocomposites: Formulation–Processing Aspects and Challenges

Selection of effective cocrystals former for dissolution rate improvement of active pharmaceutical ingredients based on lipoaffinity index

Recent Applications of Mixture Designs in Beverages, Foods, and Pharmaceutical Health: A Systematic Review and Meta-Analysis

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