Pharmaceutical particle technologies: An approach to improve drug solubility, dissolution and bioavailability

Khadka, Prakash; Ro, Jieun; Kim, Hyeongmin; Kim, Iksoo; Kim, Jeong Tae; Kim, Hyunil; Cho, Jae Min; Yun, Gyiae; Lee, Jaehwi

doi:10.1016/j.ajps.2014.05.005

Cited by 755 publications

(484 citation statements)

References 74 publications

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“…It was reported that particle size is inversely proportional to surface area. Thus, increase in particle size causes a decrease in surface area and vice versa [35]. This was also supported by the XRD data where average crystallite size of treated sample was increased that causes decrease in the surface area.…”

Section: Particle Size and Surface Area Analysissupporting

confidence: 72%

Physical, Thermal and Spectral Properties of Biofield Energy Treated 2,4-Dihydroxybenzophenone

Trivedi¹,

Tallapragada²,

Branton³

et al. 2015

Clin Pharmacol Biopharm

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Study background: 2,4-Dihydroxybenzophenone (DHBP) is an organic compound used for the synthesis of pharmaceutical agents. The objective of this study was to investigate the influence of biofield energy treatment on the physical, thermal and spectral properties of DHBP. The study was performed in two groups (control and treated). The control group remained as untreated, and the treated group received Mr. Trivedi's biofield energy treatment. Methods:The control and treated DHBP samples were further characterized by X-ray diffraction (XRD), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), laser particle size analyser, surface area analyser, Fourier transform infrared (FT-IR) spectroscopy, and ultra violet-visible spectroscopy (UV-vis) analysis. Results:The XRD study indicated a slight decrease in the volume of the unit cell and molecular weight of treated DHBP as compared to the control sample. However, XRD study revealed an increase in average crystallite size of the treated DHBP by 32.73% as compared to the control sample. The DSC characterization showed no significant change in the melting temperature of treated sample. The latent heat of fusion of the treated DHBP was substantially increased by 11.67% as compared to the control. However, TGA analysis showed a decrease in the maximum thermal decomposition temperature (T max ) of the treated DHBP (257.66 º C) as compared to the control sample (260.93 º C). The particle size analysis showed a substantial increase in particle size (d 50 and d 99 ) of the treated DHBP by 41% and 15.8% as compared to the control sample. Additionally, the surface area analysis showed a decrease in surface area by 9.5% in the treated DHBP, which was supported by the particle size results. Nevertheless, FT-IR analysis showed a downward shift of methyl group stretch (2885→2835 cm -1 ) in the treated sample as compared to the control. The UV analysis showed a blue shift of absorption peak 323→318 nm in the treated sample (T1) as compared to the control. Conclusion:Altogether, the results showed significant changes in the physical, thermal and spectral properties of treated DHBP as compared to the control.

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Section: Particle Size and Surface Area Analysissupporting

confidence: 72%

Physical, Thermal and Spectral Properties of Biofield Energy Treated 2,4-Dihydroxybenzophenone

Trivedi¹,

Tallapragada²,

Branton³

et al. 2015

Clin Pharmacol Biopharm

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“…Particle size reduction is a safe method of increasing drug dissolution without altering the chemical nature of the drug. However, although particle size reduction leads to an increase in the effective surface area of the drug available to interact with the solvent, it does not increase equilibrium solubility of the drug [11] unless the size of particles are reduced to below 1 micrometre [12]. In addition, micronization may cause agglomeration and thus may negatively impact on the solubility and bioavailability during the storage of the final product [13].…”

Section: Introductionmentioning

confidence: 99%

Solid-state, triboelectrostatic and dissolution characteristics of spray-dried piroxicam-glucosamine solid dispersions

Adebisi

Kaialy

Hussain

et al. 2016

Colloids and Surfaces B: Biointerfaces

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Solid-state, triboelectrostatic and dissolution characteristics of spray-dried piroxicam-glucosamine solid dispersions, Colloids and Surfaces B: Biointerfaces http://dx.doi.org/10. 1016/j.colsurfb.2016.07.032 This is a PDF file of an unedited manuscript that has been accepted for publication. As a service to our customers we are providing this early version of the manuscript. The manuscript will undergo copyediting, typesetting, and review of the resulting proof before it is published in its final form. Please note that during the production process errors may be discovered which could affect the content, and all legal disclaimers that apply to the journal pertain. 4. GLU improved the handling of PXM as it significantly reduced its charge in all the spray dried formulations. Technique could be used to determine appropriate formulations that improve handling AbstractThis work explores the use of both spray drying and D-glucosamine HCl (GLU) as a hydrophilic carrier to improve the dissolution rate of piroxicam (PXM) whilst investigating the electrostatic charges associated with the spray drying process. Spray dried PXM:GLU solid dispersions were prepared and characterised (XRPD, DSC, SEM). Dissolution and triboelectric charging was also conducted. The results showed that the spray dried PXM alone, without GLU produced some PXM form II (DSC results) with no enhancement in solubility relative to that of the parent PXM.XRPD results also showed the spray drying process to decrease the crystallinity of GLU and solid dispersions produced. The presence of GLU improved the dissolution rate of PXM. Spray dried PXM: GLU at a ratio of 2:1 had the most improved dissolution. The spray drying process generally yielded PXM-GLU spherical particles of around 2.5 µm which may have contributed to the improved dissolution. PXM showed a higher tendency for charging in comparison to the carrier GLU (-3.8 versus 0.5 nC/g for untreated material and -7.5 versus 3.1 nC/g for spray dried materials). Spray dried PXM and spray dried GLU demonstrated higher charge densities than untreated PXM and untreated GLU, respectively. Regardless of PXM:GLU ratio, all spray dried PXM:GLU solid dispersions showed a negligible charge density (net-CMR: 0.1 -0.3 3 nC/g). Spray drying of PXM:GLU solid dispersions can be used to produce formulation powders with practically no charge and thereby improving handling as well as dissolution behaviour of PXM.

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“…Due to the perceived advantage of small particle size (≤100nm) in increasing transmembrane permeability, nanotechnology based products are presumed to provide a significant improvement in the bioavailability of several drugs [73]. Several studies have been reported that link the biotoxicity of nanoparticles to their small particle size.…”

Section: Nanotechnology-based Approachesmentioning

confidence: 99%

Current and evolving approaches for improving the oral permeability of BCS Class III or analogous molecules

Dave

Gupta

et al. 2016

Drug Development and Industrial Pharmacy

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The Biopharmaceutics Classification System (BCS) classifies pharmaceutical compounds based on their aqueous solubility and intestinal permeability. The BCS Class III compounds are hydrophilic molecules (high aqueous solubility) with low permeability across the biological membranes. While these compounds are pharmacologically effective, poor absorption due to low permeability becomes the rate-limiting step in achieving adequate bioavailability. Several approaches have been explored and utilized for improving the permeability profiles of these compounds. The approaches include traditional methods such as prodrugs, permeation enhancers, ion-pairing, etc., as well as relatively modern approaches such as nanoencapsulation and nanosizing. The most recent approaches include a combination/hybridization of one or more traditional approaches to improve drug permeability. While some of these approaches have been extremely successful, i.e. drug products utilizing the approach have progressed through the USFDA approval for marketing; others require further investigation to be applicable. This article discusses the commonly studied approaches for improving the permeability of BCS Class III compounds. AbstractThe Biopharmaceutics Classification System (BCS) classifies pharmaceutical compounds based on their aqueous solubility and intestinal permeability. The BCS Class III compounds are hydrophilic molecules (high aqueous solubility) with low permeability across the biological membranes. While these compounds are pharmacologically effective, poor absorption due to low permeability becomes the rate-limiting step in achieving adequate bioavailability.Several approaches have been explored and utilized for improving the permeability profiles of these compounds. The approaches include traditional methods such as prodrugs, permeation enhancers, ion-pairing, etc., as well as relatively modern approaches such as nanoencapsulation and nanosizing. The most recent approaches include a combination/ hybridization of one or more traditional approaches to improve drug permeability. While some of these approaches have been extremely successful, i.e. drug products utilizing the approach have progressed through the USFDA approval for marketing; others require further investigation to be applicable. This article discusses the commonly studied approaches for improving the permeability of BCS Class III compounds.

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Pharmaceutical particle technologies: An approach to improve drug solubility, dissolution and bioavailability

Cited by 755 publications

References 74 publications

Physical, Thermal and Spectral Properties of Biofield Energy Treated 2,4-Dihydroxybenzophenone

Physical, Thermal and Spectral Properties of Biofield Energy Treated 2,4-Dihydroxybenzophenone

Solid-state, triboelectrostatic and dissolution characteristics of spray-dried piroxicam-glucosamine solid dispersions

Current and evolving approaches for improving the oral permeability of BCS Class III or analogous molecules

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