A comparative study of top-down and bottom-up approaches for the preparation of micro/nanosuspensions

Verma, Sudhir Kumar; Gokhale, Rajeev; Burgess, Diane J.

doi:10.1016/j.ijpharm.2009.07.005

Cited by 295 publications

(163 citation statements)

References 17 publications

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“…The top-down techniques apply mechanical force to reduce large particles to nanometer scale. 1 The milling or grinding technique and high-pressure homogenization technique are widely used in many research studies and in the production of commercial products. 2 The top-down techniques do not use an organic solvent; however, the processes generate heat and mechanical force that impact the surface properties.…”

Section: Introductionmentioning

confidence: 99%

Transformation of eutectic emulsion to nanosuspension fabricating with solvent evaporation and ultrasonication technique

Phaechamud

Tuntarawongsa

2016

IJN

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Eutectic solvent can solubilize high amount of some therapeutic compounds. Volatile eutectic solvent is interesting to be used as solvent in the preparation of nanosuspension with emulsion solvent evaporation technique. The mechanism of transformation from the eutectic emulsion to nanosuspension was investigated in this study. The 30% w/w ibuprofen eutectic solution was used as the internal phase, and the external phase is composed of Tween 80 as emulsifier. Ibuprofen nanosuspension was prepared by eutectic emulsion solvent evaporating method followed with ultrasonication. During evaporation process, the ibuprofen concentration in emulsion droplets was increased leading to a drug supersaturation but did not immediately recrystallize because of low glass transition temperature ( T g ) of ibuprofen. The contact angle of the internal phase on ibuprofen was apparently lower than that of the external phase at all times of evaporation, indicating that the ibuprofen crystals were preferentially wetted by the internal phase than the external phase. From calculated dewetting value ibuprofen crystallization occurred in the droplet. Crystallization of the drug was initiated with external mechanical force, and the particle size of the drug was larger due to Ostwald ripening. Cavitation force from ultrasonication minimized the ibuprofen crystals to the nanoscale. Particle size and zeta potential of formulated ibuprofen nanosuspension were 330.87±51.49 nm and −31.1±1.6 mV, respectively, and exhibited a fast dissolution. Therefore, the combination of eutectic emulsion solvent evaporation method with ultrasonication was favorable for fabricating an ibuprofen nanosuspension, and the transformation mechanism was attained successfully.

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Section: Introductionmentioning

confidence: 99%

Transformation of eutectic emulsion to nanosuspension fabricating with solvent evaporation and ultrasonication technique

Phaechamud

Tuntarawongsa

2016

IJN

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“…Nevertheless, low drug encapsulation efficiency and drug loading, residual organic solvent, especially a large amount of excipients and surfactants used in these nano-carriers will cause many side effects, such as toxicity and hemolysis. Nanosuspensions (NS) as a carrier-free submicron colloidal drug delivery system consist of pure drug with a small amount of stabilizers (Verma et al, 2009;Liu et al, 2013). By reducing particle size (PS), it confers a series of enhanced characteristics to drugs, such as the safety, stability, dissolution rate and bioavailability .…”

Section: Introductionmentioning

confidence: 99%

Nanosuspensions as delivery system for gambogenic acid: characterization and in vitro/in vivo evaluation

Yuan

Zhang

et al. 2015

Drug Delivery

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Nanosuspensions (NS) can enhance the saturation solubility and dissolution velocity of poorly soluble drugs. PEG as a non-ionic surfactant plays an important role in surface modification of nanoparticles for prolonging in vivo circulation. In this study, anti-solvent precipitation method was introduced to prepare gambogenic acid nanosuspensions (GNA-NS) with PVPK30 and PEG2000 as stabilizers to settle the disadvantages of GNA. The obtained nanoparticles were spherical with a mean particle size of 183.7 nm and a zeta potential of À22.8 mV.The entrapment efficiency and drug loading of the resultant formulation were 97.3 and 29.73%. X-ray diffraction analysis confirmed the amorphous phase of GNA in NS. Fourier transform infrared indicated there may be hydrogen bond interaction between the drug and excipients. After lyophilization of GNA-NS, the freeze-dried powder displayed sufficient longterm physical stability at 4 and 25 C. In comparison to GNA solution, in vitro studies of GNA-NS showed much slower release and higher cytotoxicity in HepG2 cells. What's more, the pharmacokinetic study in rats revealed that the AUC 0-1 and t 1/2 of GNA-NS were increased 2.63-and 1.77-fold than that of the reference formulation. Taken together, in vitro/in vivo evaluations showed NS would be an effectively strategy to change the poor aqueous solubility and prolong the half-life for GNA. The GNA-NS with enhanced bioavailability and drug efficacy provided a promising delivery system for the application of GNA. KeywordsCytotoxicity, gambogenic acid, in vivo pharmacokinetics, in vitro release, nanosuspensions History

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“…It is important to note that formulation of NS is greatly affected by technique used to prepare it, most importantly their physicochemical stability [24]. Top down method creates physical and chemical instability like crystal deformities and break down of heat labile drugs due to the generation of heat during milling process [24].…”

Section: Introductionmentioning

confidence: 99%

“…Top down method creates physical and chemical instability like crystal deformities and break down of heat labile drugs due to the generation of heat during milling process [24]. Whereas, by using bottom up technique, morphology and crystallinity of particles could be maintained.…”

Section: Introductionmentioning

confidence: 99%

“…Whereas, by using bottom up technique, morphology and crystallinity of particles could be maintained. Supercritical fluid process under bottom up technique has been used to prepare NS on large scale [22,23]; however, it suffers from certain limitations such as operation at high pressure, temperature, and requirement of fine designed nozzles [23,24]. Alternatively, solventantisolvent method has been extensively reported to prepare NS due to its simplicity and ease of scale up.…”

Section: Introductionmentioning

confidence: 99%

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Formulation of Curcumin Nanosuspension Using Box-Behnken Design and Study of Impact of Drying Techniques on Its Powder Characteristics

Kaur

Bawa

Rajesh

et al. 2017

Asian J Pharm Clin Res

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Objective: The objective of this study was to formulate curcumin nanosuspension (NS) using Box-Behnken design (BBD) and solvent-antisolvent technique to overcome the challenges related to its poor dissolution rate.Methods: Sodium lauryl sulfate (SLS) and poly vinyl pyrrolidone K-60 (PVPK-60) have been used as a surfactant and polymer, respectively, to stabilize the NS. Ethanol was used as solvent to dissolve curcumin and water was used as antisolvent. The study revealed that SLS to curcumin ratio, PVPK-60 to curcumin ratio, solvent to antisolvent ratio and speed of mixing were the critical parameters that affected particle size and zeta potential of the formulation. Hence, based on Box-BBD, 25 formulations were prepared by varying these critical parameters. The optimized batch of CRM NS was further solidified using spray drying as well as rotary evaporation techniques to have a better insight for selection of solidification process in terms of retention of particle size, charge, flow, dissolution, and stability.Results: About 39.47 folds decrease in particle size of raw CRM was observed after conversion into NS. Further, about 53.57 and 45.45 folds decrease in particle size was observed after spray drying and rotary evaporation. Both the dried nanoparticles have shown comparatively higher solubility, powder flow, and dissolution rate as that of raw CRM. Powder X-ray diffraction study revealed the formation of amorphous nanoparticles. Accelerated stability study revealed that nanoparticles dried by spray drying were able to retain the properties such as particle size, flow, and dissolution rate as compared to rotary evaporated powders. Conclusion:It can be concluded that spray drying technique could offer many advantages while loading CRM nanoparticles into tablets for their oral administration.

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A comparative study of top-down and bottom-up approaches for the preparation of micro/nanosuspensions

Cited by 295 publications

References 17 publications

Transformation of eutectic emulsion to nanosuspension fabricating with solvent evaporation and ultrasonication technique

Transformation of eutectic emulsion to nanosuspension fabricating with solvent evaporation and ultrasonication technique

Nanosuspensions as delivery system for gambogenic acid: characterization and in vitro/in vivo evaluation

Formulation of Curcumin Nanosuspension Using Box-Behnken Design and Study of Impact of Drying Techniques on Its Powder Characteristics

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