A Brief Literature and Patent Review of Nanosuspensions to a Final Drug Product

Chin, William W.; Parmentier, Johannes; Widzinski, Michael; Tan, En Hui; Gokhale, Rajeev

doi:10.1002/jps.24098

Cited by 82 publications

(38 citation statements)

References 141 publications

(159 reference statements)

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“…The publication analysis performed by Lim Chin et al . indicated that about 22% of the total development in the context of nanosuspensions focused on ophthalmic and nasal drug delivery. The nano‐ and micro‐sized carriers from drug/CD complex aggregates, using natural CDs, were developed by Loftsson and coworkers .…”

Section: Cyclodextrin‐based Nanocarriers For Targeted Ocular and Nasamentioning

confidence: 99%

“…Structurally tailored CDs have led to special nanoarchitectures, such as nanospheres, nanomicelles, nanoparticles and nanogels, with either water-soluble or insoluble drugs being loaded into the hydrophilic and hydrophobic parts of the CD units. The publication analysis performed by Lim Chin et al [82] indicated that about 22% of the total development in the context of nanosuspensions focused on ophthalmic and nasal drug delivery. The nano-and micro-sized carriers from drug/CD complex aggregates, using natural CDs, were developed by Loftsson and coworkers [83].…”

Section: Cyclodextrin-based Nanocarriers For Targeted Ocular and Nasamentioning

confidence: 99%

See 1 more Smart Citation

Cyclodextrin‐Based Formulations: A Non‐Invasive Platform for Targeted Drug Delivery

Muankaew

Loftsson

2017

Basic Clin Pharma Tox

156

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Cyclodextrins (CDs) are recognized as promising pharmaceutical excipients due to their unique ability to form watersoluble inclusion complexes with various poorly soluble compounds. The numerous investigations on CDs and their use in nanomedicine have received considerable attention in the last three decades, leading to the rapid development of new CD-containing formulations that significantly facilitate targeted drug delivery and controlled drug release, with consequent improvements in drug bioavailability. This MiniReview highlights the efficacy and recent uses of CDs for non-invasive drug delivery. Using ophthalmic and nasal drug delivery as examples, an overview of chemical properties, mechanisms of CDs on drug solubilization, stabilization and permeation, along with their toxicological profiles relevant to nasal and ocular administration, are provided and discussed. The recent development and application of CD-based nanocarrier systems for targeted drug delivery are summarized.Cyclodextrins (CDs) are natural cyclic oligosaccharides that are produced by enzymatic degradation of starch. There are three native CDs designated aCD, bCD and cCD, which are composed of 6, 7 and 8 D-glucopyranose units linked by a-(1, 4) glycosidic, respectively [1]. The molecules are commonly described as truncated cone, bucket-like or donut-shaped, with a hydrophilic outer surface and a relatively hydrophobic inner cavity that allows entrapment of small hydrophobic drug molecules or hydrophobic moieties of larger molecules [2], thereby providing drugs with new physicochemical characteristics without altering their intrinsic properties. Table 1 summarizes the characteristics of different CDs. Natural CDs are preferred for complexation; however, their usability is limited by the small cavity size of aCD, poor aqueous solubility of bCD and low productivity of cCD [3]. Derivatized CDs can be obtained by substituting their hydroxyl groups with desired functional moieties. Methyl-(MebCD and MecCD) [4,5], hydroxypropyl-(HPaCD, HPbCD and HPcCD) [6][7][8] and sulphobutylether (SEBbCD) derivatives [9] are frequently found in pharmaceutical products and have improved solubility and inclusion capacity over natural CDs. Pharmaceutical applications of both natural CDs and their derivatives are common when drug/CD complexes are used to increase drug solubility, improve organoleptic properties [10], enhance drug permeation [11] and increase drug stability, resulting in increased product shelf-life and drug bioavailability [12]. In addition, spontaneous self-assembly of drug/CD complexes into aggregates can lead to innovative drug delivery systems, such as CD-containing liposomes and microspheres as well as microand nanoparticles [13]. Polymerized CDs (e.g. Epi-aCD and Epi-bCD) have also been synthesized to enhance the selfassembly ability of CDs, and to strengthen their interactions with drugs and biological membranes [14]. Compared with other pharmaceutical excipients, CDs have been shown to reduce the toxicity of several drugs and are...

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Section: Cyclodextrin‐based Nanocarriers For Targeted Ocular and Nasamentioning

confidence: 99%

Section: Cyclodextrin-based Nanocarriers For Targeted Ocular and Nasamentioning

confidence: 99%

Cyclodextrin‐Based Formulations: A Non‐Invasive Platform for Targeted Drug Delivery

Muankaew

Loftsson

2017

Basic Clin Pharma Tox

156

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“…All aforementioned techniques have their own advantages and limitations 7 . Among these techniques, nanonization is one of the widely used technique for improvement in solubility and bioavailability, as evidenced by huge literature and approved marketed products such as Rapamune ® , Emend ® , Triglide ® , Tricor ® , Megace ES ® already available in market 8 . Recent reports on the current market scenario of nanocrystals claim that it will occupy around 60% of a $136 billion nanotechnology-enabled drug delivery market by 2021 9 .…”

Section: Introductionmentioning

confidence: 99%

Parenteral nanosuspensions: a brief review from solubility enhancement to more novel and specific applications

Ahire

Thakkar

Darshanwad

et al. 2018

Acta Pharmaceutica Sinica B

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Advancements in in silico techniques of lead molecule selection have resulted in the failure of around 70% of new chemical entities (NCEs). Some of these molecules are getting rejected at final developmental stage resulting in wastage of money and resources. Unfavourable physicochemical properties affect ADME profile of any efficacious and potent molecule, which may ultimately lead to killing of NCE at final stage. Numerous techniques are being explored including nanocrystals for solubility enhancement purposes. Nanocrystals are the most successful and the ones which had a shorter gap between invention and subsequent commercialization of the first marketed product. Several nanocrystal-based products are commercially available and there is a paradigm shift in using approach from simply being solubility enhancement technique to more novel and specific applications. Some other aspects in relation to parenteral nanosuspensions are concentrations of surfactant to be used, scalability and in vivo fate. At present, there exists a wide gap due to poor understanding of these critical factors, which we have tried to address in this review. This review will focus on parenteral nanosuspensions, covering varied aspects especially stabilizers used, GRAS (Generally Recognized as Safe) status of stabilizers, scalability challenges, issues of physical and chemical stability, solidification techniques to combat stability problems and in vivo fate.

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“…To characterize the particle surfaces, the particle size distribution and the zeta potential of the resveratrol nanosuspension were measured using a dynamic light scattering (DLS) instrument (ELSZ-1000; Photal Otsuka Electronics, Osaka, Japan) at 25 • C. Particle size was measured in triplicate and expressed as the z-average diameter. DLS was employed to determine the particle size and its distribution of the nanoparticles in suspension [26]. The zeta potential is a measure of the electric charge at the surface of the particles and is used to indicate the physical stability of colloidal systems.…”

Section: Measurement Of Particle Size and Zeta Potentialmentioning

confidence: 99%

“…One of the major problems with nanosuspensions is the difference in saturation solubility and concentration gradient, which can lead to Ostwald ripening [26]. This phenomenon can be controlled using various additives.…”

Section: Screening For Stabilizersmentioning

confidence: 99%

Development of a Resveratrol Nanosuspension Using the Antisolvent Precipitation Method without Solvent Removal, Based on a Quality by Design (QbD) Approach

Kuk

et al. 2019

Pharmaceutics

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The purpose of this study was to develop a resveratrol nanosuspension with enhanced oral bioavailability, based on an understanding of the formulation and process parameters of nanosuspensions and using a quality by design (QbD) approach. Particularly, the antisolvent method, which requires no solvent removal and no heating, is newly applied to prepare resveratrol nanosuspension. To ensure the quality of the resveratrol nanosuspensions, a quality target product profile (QTPP) was defined. The particle size (z-average, d90), zeta potential, and drug content parameters affecting the QTPP were selected as critical quality attributes (CQAs). The optimum composition obtained using a 3-factor, 3-level Box–Behnken design was as follows: polyvinylpyrrolidone vinyl acetate (10 mg/mL), polyvinylpyrrolidone K12 (5 mg/mL), sodium lauryl sulfate (1 mg/mL), and diethylene glycol monoethyl ether (DEGEE, 5% v/v) at a resveratrol concentration of 5 mg/mL. The initial particle size (z-average) was 46.3 nm and the zeta potential was −38.02 mV. The robustness of the antisolvent process using the optimized composition conditions was ensured by a full factorial design. The dissolution rate of the optimized resveratrol nanosuspension was significantly greater than that of the resveratrol raw material. An in vivo pharmacokinetic study in rats showed that the area under the plasma concentration versus time curve (AUC0–12h) and the maximum plasma concentration (Cmax) respectively, than those of the resveratrol raw material. Therefore, the prepara values of the resveratrol nanosuspension were approximately 1.6- and 5.7-fold higher,tion of a resveratrol nanosuspension using the QbD approach may be an effective strategy for the development of a new dosage form of resveratrol, with enhanced oral bioavailability.

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A Brief Literature and Patent Review of Nanosuspensions to a Final Drug Product

Cited by 82 publications

References 141 publications

Cyclodextrin‐Based Formulations: A Non‐Invasive Platform for Targeted Drug Delivery

Cyclodextrin‐Based Formulations: A Non‐Invasive Platform for Targeted Drug Delivery

Parenteral nanosuspensions: a brief review from solubility enhancement to more novel and specific applications

Development of a Resveratrol Nanosuspension Using the Antisolvent Precipitation Method without Solvent Removal, Based on a Quality by Design (QbD) Approach

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