A formulation comparison, using a solution and different nanosuspensions of a poorly soluble compound

Sigfridsson, Kalle; Forssén, Sara; Hollander, P. H. C. den; Skantze, Urban; Verdier, Jennie de

doi:10.1016/j.ejpb.2007.02.008

Cited by 61 publications

(24 citation statements)

References 28 publications

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“…This difference may counterbalance the driving force for Ostwald ripening and eventually result in a termination (16). There are reports stating that hydrophobic substances with a low hydrophilic-lipophilic balance (HLB) value act as Ostwald ripening inhibitors (17). Nonionic stabilizers can be hydrophilic with higher HLB values (8~18) or lipophilic with HLB values in the range 1~8.…”

Section: Introductionmentioning

confidence: 99%

“…Nanosuspensions can have drug particulates in crystalline or amorphous state. The nanoprecipitation process is reported to yield amorphous suspensions (16,17). Amorphous drug nanosuspensions are prone to particle growth due to Ostwald ripening which is a process where the difference in local solubility with particle size leads to a transport of material from small to larger particles, with an accompanying increase in the mean particle size with time.…”

Section: Introductionmentioning

confidence: 99%

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Silver Sulfadiazine Nanosystems for Burn Therapy

Venkataraman

Nagarsenker

2012

AAPS PharmSciTech

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Abstract. The objective of the present study was to formulate stable silver sulfadiazine (SSD) nanosuspensions and nanogels suitable for topical delivery with a view to increase bactericidal activity in burn therapy. SSD nanosuspensions were formulated using the microprecipitation-high-pressure homogenization technique. An optimized microsuspension of 0.5% SSD formulated with 6% Cremophor EL and 4% Lauroglycol 90 was subjected to 30 cycles of 1,000-bar pressure to give a nanosuspension with an average particle size of 367.85 nm. Transmission electron microscopy studies revealed that ovoid-to rectangularshaped SSD particles were present as clusters. It was evident through X-ray diffraction studies that SSD was present in amorphous state both in microprecipitate and in nanosuspension. SSD (0.5%) nanogels were prepared using 1% Carbopol 974 P for topical delivery of nanosized SSD. In vitro release studies demonstrated that SSD release was faster from solutions and nanosuspensions compared to gel formulation owing to the influence of the gel matrix on SSD release. The bacterial inhibitory efficiency of SSD nanosuspension was as good as that of SSD solution against Staphylococcus aureus, Escherichia coli, and Pseudomonas aeruginosa. In vivo studies revealed that a nanogel containing 0.5% SSD was more effective in wound healing compared to 0.5% and 1% marketed cream.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Silver Sulfadiazine Nanosystems for Burn Therapy

Venkataraman

Nagarsenker

2012

AAPS PharmSciTech

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“…Similarly, the pharmacokinetics of AZ68, a poorly soluble compound, when administered intravenously as a solution or as a nanosuspension was similar; AZ68 is approximately five times less soluble than ticagrelor at physiological pH. 34 In the present study, the plasma concentrations after intravenous administration of ticagrelor nanosuspensions were less than the exposures obtained after oral administration to rats and dogs. 27 This observation suggests that the ticagrelor particles dissolved upon dilution in blood allow for a solution-like distribution.…”

Section: Discussionmentioning

confidence: 52%

Usefulness of a Nanoparticle Formulation to Investigate Some Hemodynamic Parameters of a Poorly Soluble Compound

Sigfridsson

Björkman

Skantze

et al. 2011

Journal of Pharmaceutical Sciences

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“…Most of these approaches require more than 100 mg API per batch, assuming an API content of 10 wt % [13,[15][16][17]. Other approaches are operating with atmospheric air in the milling chamber [18][19][20], which can lead to foaming during processing, especially when using stabilizers with high foaming tendency like polyvinyl alcohol or hydroxypropyl cellulose. The multi-well approach [21] was identified as well, with limitations for its practical use due to deformation and wear [19].…”

Section: Introductionmentioning

confidence: 99%

Accelerated Formulation Development for Nanomilled Active Pharmaceutical Ingredients Using a Screening Approach

2010

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In order to enable the accelerated preclinical and clinical pharmaceutical development of formulations based on nanomilling, a screening media mill was developed and evaluated for the production of nanoparticulate active pharmaceutical ingredients (API). The screening media mill is based on the principle of a conventional planetary mill, equipped with up to 24 milling beakers of 0.05-1.0 mL individual milling chamber volume. The applicability of the screening media mill was evaluated by 0.7-12.8 mg naproxen (2 wt %) per batch with a nanomilling formulation known from the literature. A case study for the preclinical formulation development is presented, applying 42 screening experiments by one operator within 5 working days, using in total 110 mg API. Promising nanomilling formulations with median particle sizes below 200 nm could be identified, suitable for preclinical in vivo studies. A second case study for the early clinical development of another proprietary API showed the successful formulation development within 12 working days. Up-scaling to a miniaturized stirred media mill of 10 mL milling chamber volume resulted in a satisfying comparability of the selected formulations, with varying performance. Further up-scaling of the most promising formulation to a laboratory-scale stirred-media mill showed the successful production of 250 g API with a median particle size of 140 nm.

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A formulation comparison, using a solution and different nanosuspensions of a poorly soluble compound

Cited by 61 publications

References 28 publications

Silver Sulfadiazine Nanosystems for Burn Therapy

Silver Sulfadiazine Nanosystems for Burn Therapy

Usefulness of a Nanoparticle Formulation to Investigate Some Hemodynamic Parameters of a Poorly Soluble Compound

Accelerated Formulation Development for Nanomilled Active Pharmaceutical Ingredients Using a Screening Approach

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