Nanocrystallization of Poorly Water Soluble Drugs for Parenteral Administration

Zakir, Foziyah; Sharma, Himanshu; Kaur, Karandeep; Malik, Basant; Vaidya, Bhuvaneshwer; Goyal, Amit K.; Vyas, Sameer

doi:10.1166/jbn.2011.1234

Cited by 7 publications

(3 citation statements)

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“…On similar lines, Zakir et al 134 recently reported amphotericin B nanocrystal-based formulation for parenteral administration. They have used Tween 80, Pluronic ® F68 and Soya lecithin as the stabilizers to achieve stability and desired particle size range.…”

Section: Parenteral Nanosuspensionmentioning

confidence: 84%

“…They have used Tween 80, Pluronic ® F68 and Soya lecithin as the stabilizers to achieve stability and desired particle size range. Nanocrystal formulation for the parenteral administration with smaller particle size was successfully produced with the NanoEdge TM technology 134 . The technology utilizes basic precipitation process followed by annealing step applying high energy either in the form of shear or thermal energies 33 .…”

Section: Parenteral Nanosuspensionmentioning

confidence: 99%

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

Ahire

Thakkar

Darshanwad

et al. 2018

Acta Pharmaceutica Sinica B

105

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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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Section: Parenteral Nanosuspensionmentioning

confidence: 84%

Section: Parenteral Nanosuspensionmentioning

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

105

View full text Add to dashboard Cite

show abstract

“…The number of poorly soluble drug compounds has increased sharply since high-throughput screening and combinatorial chemistry were introduced into pharmaceutical development processes. [ 1 2 3 ] Enhancing the oral bioavailability of poorly water-soluble drugs by an increasing dissolution is one of the most challenging tasks in drug development. [ 4 5 ] The various methods such as salt formation, solubilization, particle-size reduction, and solid dispersion (SD) formation have been reported for this purpose.…”

Section: Introductionmentioning

confidence: 99%

Enhanced dissolution and stability of Tanshinone IIA base by solid dispersion system with nano-hydroxyapatite

Jiang¹,

Zhang²,

Saiyan³

et al. 2014

Phcog Mag

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Background:Tanshinone IIA (TSIIA) exhibits a variety of cardiovascular effects; however, it has low solubility in water. The preparation of poorly soluble drugs for oral delivery is one of the greatest challenges in the field of formulation research. Among the approaches available, solid dispersion (SD) technique has proven to be one of the most commonly used these methods for improving dissolution and bioavailability of drugs, because of its relative simplicity and economy in terms of both preparation and evaluation.Objective:This study was aimed at investigating the dissolution behavior and physical stability of SDs of TSIIA by employing nano-hydroxyapatite (n-HAp).Materials and Methods:The TSIIA SDs was prepared to use a spray-drying method. First, an in vitro dissolution test was performed to assess dissolution characteristics. Next, a set of complementary techniques (differential scanning calorimetry, scanning electron microscopy, X-ray powder diffraction, and Fourier transform infrared spectroscopy) was used to monitor the physicochemical properties of the SDs. The SDs was stored at 40°C/75% relative humidity for 6 months, after which their stability was assessed.Results:TSIIA dissolution remarkably improved because of the formulation of the SDs with n-HAp particles. Comparisons with the corresponding physical mixtures revealed changes in the SDs and explained the formation of the amorphous phase. In the stability test, virtually no time-dependent decrease was observed in either in vitro drug dissolution or drug content.Conclusion:SD formulation with n-HAp may be a promising approach for enhancing the dissolution and stability of TSIIA.

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Mechanisms of extracellular vesicle uptake and implications for the design of cancer therapeutics

Jackson Cullison,

Flemming,

Karagoz

et al. 2024

J of Extracellular Bio

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The translation of pre‐clinical anti‐cancer therapies to regulatory approval has been promising, but slower than hoped. While innovative and effective treatments continue to achieve or seek approval, setbacks are often attributed to a lack of efficacy, failure to achieve clinical endpoints, and dose‐limiting toxicities. Successful efforts have been characterized by the development of therapeutics designed to specifically deliver optimal and effective dosing to tumour cells while minimizing off‐target toxicity. Much effort has been devoted to the rational design and application of synthetic nanoparticles to serve as targeted therapeutic delivery vehicles. Several challenges to the successful application of this modality as delivery vehicles include the induction of a protracted immune response that results in their rapid systemic clearance, manufacturing cost, lack of stability, and their biocompatibility. Extracellular vesicles (EVs) are a heterogeneous class of endogenous biologically produced lipid bilayer nanoparticles that mediate intercellular communication by carrying bioactive macromolecules capable of modifying cellular phenotypes to local and distant cells. By genetic, chemical, or metabolic methods, extracellular vesicles (EVs) can be engineered to display targeting moieties on their surface while transporting specific cargo to modulate pathological processes following uptake by target cell populations. This review will survey the types of EVs, their composition and cargoes, strategies employed to increase their targeting, uptake, and cargo release, and their potential as targeted anti‐cancer therapeutic delivery vehicles.

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Nanocrystallization of Poorly Water Soluble Drugs for Parenteral Administration

Cited by 7 publications

References 0 publications

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

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

Enhanced dissolution and stability of Tanshinone IIA base by solid dispersion system with nano-hydroxyapatite

Mechanisms of extracellular vesicle uptake and implications for the design of cancer therapeutics

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