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      • Record: found
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      Liquisolid technique and its applications in pharmaceutics

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          Abstract

          Most of the newly developed drug candidates are lipophilic and poorly water-soluble. Enhancing the dissolution and bioavailability of these drugs is a major challenge for the pharmaceutical industry. Liquisolid technique, which is based on the conversion of the drug in liquid state into an apparently dry, non-adherent, free flowing and compressible powder, is a novel and advanced approach to tackle the issue. The objective of this article is to present an overview of liquisolid technique and summarize the progress of its applications in pharmaceutics. Low cost, simple processing and great potentials in industrial production are main advantages of this approach. In addition to the enhancement of dissolution rate of poorly water-soluble drugs, this technique is also a fairly new technique to effectively retard drug release. Furthermore, liquisolid technique has been investigated as a tool to minimize the effect of pH variation on drug release and as a promising alternative to conventional coating for the improvement of drug photostability in solid dosage forms. Overall, liquisolid technique is a newly developed and promising tool for enhancing drug dissolution and sustaining drug release, and its potential applications in pharmaceutics are still being broadened.

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          Oral bioavailability of cyclosporine: solid lipid nanoparticles (SLN) versus drug nanocrystals.

          S Runge-Ranzinger, R Müller, V Ravelli … (2006)
          For the development of an optimized oral formulation for cyclosporine A, 2% of this drug has been formulated in solid lipid nanoparticles (SLN, mean size 157 nm) and as nanocrystals (mean size 962 nm). The encapsulation rate of SLN was found to be 96.1%. Nanocrystals are composed of 100% of drug. For the assessment of the pharmacokinetic parameters the developed formulations have been administered via oral route to three young pigs. Comparison studies with a commercial Sandimmun Neoral/Optoral used as reference have been performed. The blood profiles observed after oral administration of the commercial microemulsion Sandimmun revealed a fast absorption of drug leading to the observation of a plasma peak above 1,000 ng/ml within the first 2 h. For drug nanocrystals most of the blood concentrations were in the range between 30 and 70 ng/ml over a period of 14 h. These values were very low, showing huge differences between the measuring time points and between the tested animals. On the contrary, administration of cyclosporine-loaded SLN led to a mean plasma profile with almost similarly low variations in comparison to the reference microemulsion, however with no initial blood peak as observed with the Sandimmun Neoral/Optoral. Comparing the area under the curves (AUC) obtained with the tested animals it could be stated that the SLN formulation avoids side effects by lacking blood concentrations higher than 1,000 ng/ml. In this study it has been proved that using SLN as a drug carrier for oral administration of cyclosporine A a low variation in bioavailability of the drug and simultaneously avoiding the plasma peak typical of the first Sandimmun formulation can be achieved.
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            When poor solubility becomes an issue: from early stage to proof of concept.

            H Ogier, H Linden, S Stegemann … (2007)
            Drug absorption, sufficient and reproducible bioavailability and/or pharmacokinetic profile in humans are recognized today as one of the major challenges in oral delivery of new drug substances. The issue arose especially when drug discovery and medicinal chemistry moved from wet chemistry to combinatorial chemistry and high throughput screening in the mid-1990s. Taking into account the drug product development times of 8-12 years, the apparent R&D productivity gap as determined by the number of products in late stage clinical development today, is the result of the drug discovery and formulation development in the late 1990s, which were the early and enthusiastic times of the combinatorial chemistry and high throughput screening. In parallel to implementation of these new technologies, tremendous knowledge has been accumulated on biological factors like transporters, metabolizing enzymes and efflux systems as well as on the physicochemical characteristics of the drug substances like crystal structures and salt formation impacting oral bioavailability. Research tools and technologies have been, are and will be developed to assess the impact of these factors on drug absorption for the new chemical entities. The conference focused specifically on the impact of compounds with poor solubility on analytical evaluation, prediction of oral absorption, substance selection, material and formulation strategies and development. The existing tools and technologies, their potential utilization throughout the drug development process and the directions for further research to overcome existing gaps and influence these drug characteristics were discussed in detail.
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              Enhanced absorption of the poorly soluble drug fenofibrate by tuning its release rate from ordered mesoporous silica.

              P Annaert, Jan van Lanschot, Patrick Augustijns … (2010)
              The aim of the present study was to evaluate the effect of release rate from ordered mesoporous silica materials on the rate and extent of absorption of the poorly soluble drug fenofibrate. Three ordered mesoporous silica materials with different pore diameter (7.3 nm, 4.4 nm and 2.7 nm) were synthesized and loaded with fenofibrate via impregnation. Release experiments were conducted under sink conditions and under supersaturating conditions in biorelevant media, simulating the fasted and the fed state. Subsequently, all silica-based formulations were evaluated in vivo (rat model). The release experiments under sink conditions indicated a clear increase in release rate with increasing pore size. However, under supersaturating conditions (FaSSIF), the, pharmaceutical performance (in terms of both the degree and duration of supersaturation), increased with decreasing pore size. The same trend was observed in vivo (fasted state): the area under the plasma concentration-time profile amounted to 102 ± 34 μMh, 86 ± 19 μMh and 20 ± 13 μMh for the materials with pore diameter of 2.7 nm, 4.4 nm and 7.3 nm, respectively. The results of this, study demonstrate that a decrease in drug release rate - and thus, a decrease of the rate at which supersaturation is created - is beneficial to the absorption of fenofibrate. Copyright © 2010 Elsevier B.V. All rights reserved.
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                Author and article information

                Contributors
                Dongkai Wang
                Pingtian Ding
                Journal
                Journal ID (nlm-ta): Asian J Pharm Sci
                Journal ID (iso-abbrev): Asian J Pharm Sci
                Title: Asian Journal of Pharmaceutical Sciences
                Publisher: Shenyang Pharmaceutical University
                ISSN (Print): 1818-0876
                ISSN (Electronic): 2221-285X
                Publication date PMC-release: 04 November 2016
                Publication date (Print): March 2017
                Publication date (Electronic): 04 November 2016
                Volume: 12
                Issue: 2
                Pages: 115-123
                Affiliations
                [a ]School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, China
                [b ]Department of Basic Pharmaceutical Sciences, School of Pharmacy, Husson University, Bangor, ME, USA
                Author notes
                [* ]Corresponding author. Shenyang Pharmaceutical University, No.103, Wenhua Road, Shenyang 110016, China. Fax: +86 24 23986310. Wangdksy@ 123456126.com
                [** ]Corresponding author. Shenyang Pharmaceutical University, No.103, Wenhua Road, Shenyang 110016, China. Fax: +86 24 23986305. dingpingtian@ 123456qq.com
                Article
                Publisher ID: S1818-0876(16)30172-6
                DOI: 10.1016/j.ajps.2016.09.007
                PMC ID: 7032177
                SO-VID: ad25e959-8f2e-4e40-804a-f17bab39b459
                Copyright © © 2017 Shenyang Pharmaceutical University. Production and hosting by Elsevier B.V.
                License:

                This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).

                History
                Date received : 18 April 2016
                Date revision received : 11 September 2016
                Date accepted : 27 September 2016
                Categories
                Subject: Review Article

                Keywords: liquisolid technique,dissolution enhancement,poorly water-soluble drugs,sustained release,ph variation,photostability
                Data availability:
                Keywords: liquisolid technique, dissolution enhancement, poorly water-soluble drugs, sustained release, ph variation, photostability

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