Naproxen-Gelucire Nanoformulations for Improved Solubility and Dissolution Rate of Poorly Water-Soluble Drug Naproxen

Sandeep Patnaik; Aditya Dileep Kurdekar; Lakshmi Adinarayana Avinash Chunduri; Chinnakoti Prathibha; Kamisetti Venkataramaniah

doi:doi:10.11648/j.jddmc.20170306.11

Naproxen-Gelucire Nanoformulations for Improved Solubility and Dissolution Rate of Poorly Water-Soluble Drug Naproxen

Sandeep Patnaik, Aditya Dileep Kurdekar, Lakshmi Adinarayana Avinash Chunduri, Chinnakoti Prathibha, Kamisetti Venkataramaniah

Published in Journal of Drug Design and Medicinal Chemistry (Volume 3, Issue 6)

Received: 23 June 2017 Accepted: 25 October 2017 Published: 23 November 2017

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Abstract

Naproxen-Gelucire Nanoformulations (NFs) in terms of their phase solubility behavior, physico-chemical characteristics, cytotoxicity and morphology and dissolution enhancement has been studied using the poorly water soluble drug, naproxen. The NFs were prepared via wet milling using a conventional Retsch Planetary ball mill in various ratios of drug to polymer (1:1, 1:2, 1:3, 1:4). The release rate of naproxen from various ratios of drug/polymer nanoparticles was investigated using USP paddle apparatus (type II). A comparative phase solubility of naproxen was performed in different carrier concentrations of simulated gastric fluid (pH 1.2) and simulated intestinal fluid (pH 6.8). The highest dissolution enhancement was achieved for the formulation with ratio of 1:4. This is a 160% enhancement when compared to that of the pure drug. The ability of amphiphillic surfactant carriers to accelerate in vitro dissolution of poorly water-soluble drugs has been attributed to wetting, micellar solubilization, and/or deflocculation. The Korsemeyer–Peppas model most aptly fits the in vitro dissolution data and gives an insight into the possible drug release mechanisms predominated by anamolous non-Fickian diffusion. Thus, the nanoformulations studied can help improve the physicochemical characteristics of naproxen towards its dissolution enhancement and possibly will increase the oral bioavailability of the drug without any adverse cytotoxic consequences.

Published in	Journal of Drug Design and Medicinal Chemistry (Volume 3, Issue 6)
DOI	10.11648/j.jddmc.20170306.11
Page(s)	77-85
Creative Commons	This is an Open Access article, distributed under the terms of the Creative Commons Attribution 4.0 International License (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution and reproduction in any medium or format, provided the original work is properly cited.
Copyright	Copyright © The Author(s), 2017. Published by Science Publishing Group

Keywords

Naproxen, Gelucire, Nanoformulations, Solubility, Dissolution, Bioavalability

References

[1]	Harrington P. J. & Lodewijk, E. (1997) Twenty, Years of Naproxen Technology. Org. Process Res. Dev. 1, 72–76.
[2]	Global and Chinese Naproxen (CAS22204-53-1) Industry-2015 http://www.researchandmarkets.com/reports/3343235/ Global.
[3]	Mura, P., Faucci, M. T., Manderioli, a, Bramanti, G. & Parrini, P. (1999), Thermal behavior and dissolution properties of naproxen from binary and ternary solid dispersions. Drug Dev. Ind. Pharm. 25, 257–64.
[4]	Mura, P., Faucci, M. T. & Bettinetti, G. P. (2001), The influence of polyvinylpyrrolidone on naproxen complexation with hydroxypropyl-??-cyclodextrin. Eur. J. Pharm. Sci. 13, 187–194.
[5]	Mura, P. et al. (2005) Interaction of naproxen with ionic cyclodextrins in aqueous solution and in the solid state. J. Pharm. Biomed. Anal. 37, 987–994.
[6]	Mura, P. et al (2005) Solid-state characterization and dissolution properties of Naproxen-Arginine-Hydroxypropyl-cyclodextrin ternary system. Eur. J. Pharm. Biopharm. 59, 99–106.
[7]	Tiong, N. & Elkordy, A. A. (2009), Effects of liquisolid formulations on dissolution of naproxen. Eur. J. Pharm. Biopharm. 73, 373–384.
[8]	Lee, B. J. & Lee, J. R. (1995) Enhancement of solubility and dissolution rate of poorly water- soluble naproxen by complexation with 2-hydroxypropyl-beta- cyclodextrin. Arch. Pharm. Res. 18, 22–26.
[9]	Allesø, M. et al. (2009) Enhanced dissolution rate and synchronized release of drugs in binary systems through formulation: Amorphous naproxen-cimetidine mixtures prepared by mechanical activation. J. Control. Release 136, 45–53.
[10]	Bogdanova, S., Pajeva, I., Nikolova, P., Tsakovska, I. & Müller, B. (2005) Interactions of poly(vinylpyrrolidone) with ibuprofen and naproxen: experimental and modeling studies. Pharm. Res., 22, 806–15.
[11]	Javadzadeh, Y. et al. (2010) Preparation and physicochemical characterization of naproxen-PLGA nanoparticles. Colloids Surf. B. Biointerfaces 81, 498–502.
[12]	Liversidge, G. G. & Conzentino, P. 1(995) Drug particle size reduction for decreasing gastric irritancy and enhancing absorption of naproxen in rats. Int. J. Pharm. 125, 309–313.
[13]	Müller, R. H., Jacobs, C. & Kayser, O. (2001) Nanosuspensions as particulate drug formulations in therapy: Rationale for development and what we can expect for the future. Adv. Drug Deliv. Rev. 47, 3–19.
[14]	Patravale, V. B., Date, A. a & Kulkarni, R. M.(2004) Nanosuspensions: a promising drug delivery strategy. J. Pharm. Pharmacol. 56, 827–40.
[15]	Bhakay, A., Merwade, M., Bilgili, E. & Dave, R. N.(2011) Novel aspects of wet milling for the production of microsuspensions and nanosuspensions of poorly water-soluble drugs. Drug Dev. Ind. Pharm. 37, 963–976.
[16]	George, M. & Ghosh, I. (2013) Identifying the correlation between drug/stabilizer properties and critical quality attributes (CQAs) of nanosuspension formulation prepared by wet media milling technology. Eur. J. Pharm. Sci. 48, 142–152.
[17]	Ghosh, I. & Michniak-Kohn, B.(2012) Design and characterization of submicron formulation for a poorly soluble drug: The effect of Vitamin e TPGS and other solubilizers on skin permeability enhancement. Int. J. Pharm. 434, 90–98.
[18]	Reintjes, T.(2011) Solubility Enhancement with BASF Pharma Polymers Solubilizer Compendium. October.
[19]	Patnaik, S., Aditha, S. K., Rattan, T. & Kamisetti, V.(2015) Aceclofenac-Soluplus Nanocomposites for Increased Bioavailability. Soft Nanosci. Lett. 5, 13–20.
[20]	Noyes A. A, Whitney W. R. (1897) The rate of solution of solid substances in their own solutions. J. Am. Chem. Soc. 19: 930-934.
[21]	Florez-Zamora, M. I. et al. (2008) Comparative study of Al-Ni-Mo alloys obtained by mechanical alloying in different ball mills. Rev. Adv. Mater. Sci. 18, 301–304.
[22]	Ahuja, N., Katare, O. P. & Singh, B.(2007) Studies on dissolution enhancement and mathematical modeling of drug release of a poorly water-soluble drug using water-soluble carriers. Eur. J. Pharm. Biopharm. 65, 26–38.
[23]	Maulvi, F. a. et al. (2007) Improvement of dissolution rate of aceclofenac by solid dispersion technique. Powder Technol. 207, 218–226.
[24]	Higuchi, T. & Connors, K. A. (1965) Phase-Solubility Techniques. Adv. Anal. Chem. Instrum. 4, 117–210 (1965).
[25]	Korsmeyer, R. W., Gurny, R., Doelker, E., Buri, P. & Peppas, N. A. (1983) Mechanisms of solute release from porous hydrophilic polymers. Int. J. Pharm. 15, 25–35.

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APA Style

Sandeep Patnaik, Aditya Dileep Kurdekar, Lakshmi Adinarayana Avinash Chunduri, Chinnakoti Prathibha, Kamisetti Venkataramaniah. (2017). Naproxen-Gelucire Nanoformulations for Improved Solubility and Dissolution Rate of Poorly Water-Soluble Drug Naproxen. Journal of Drug Design and Medicinal Chemistry, 3(6), 77-85. https://doi.org/10.11648/j.jddmc.20170306.11

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ACS Style

Sandeep Patnaik; Aditya Dileep Kurdekar; Lakshmi Adinarayana Avinash Chunduri; Chinnakoti Prathibha; Kamisetti Venkataramaniah. Naproxen-Gelucire Nanoformulations for Improved Solubility and Dissolution Rate of Poorly Water-Soluble Drug Naproxen. J. Drug Des. Med. Chem. 2017, 3(6), 77-85. doi: 10.11648/j.jddmc.20170306.11

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AMA Style

Sandeep Patnaik, Aditya Dileep Kurdekar, Lakshmi Adinarayana Avinash Chunduri, Chinnakoti Prathibha, Kamisetti Venkataramaniah. Naproxen-Gelucire Nanoformulations for Improved Solubility and Dissolution Rate of Poorly Water-Soluble Drug Naproxen. J Drug Des Med Chem. 2017;3(6):77-85. doi: 10.11648/j.jddmc.20170306.11

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@article{10.11648/j.jddmc.20170306.11,
  author = {Sandeep Patnaik and Aditya Dileep Kurdekar and Lakshmi Adinarayana Avinash Chunduri and Chinnakoti Prathibha and Kamisetti Venkataramaniah},
  title = {Naproxen-Gelucire Nanoformulations for Improved Solubility and Dissolution Rate of Poorly Water-Soluble Drug Naproxen},
  journal = {Journal of Drug Design and Medicinal Chemistry},
  volume = {3},
  number = {6},
  pages = {77-85},
  doi = {10.11648/j.jddmc.20170306.11},
  url = {https://doi.org/10.11648/j.jddmc.20170306.11},
  eprint = {https://article.sciencepublishinggroup.com/pdf/10.11648.j.jddmc.20170306.11},
  abstract = {Naproxen-Gelucire Nanoformulations (NFs) in terms of their phase solubility behavior, physico-chemical characteristics, cytotoxicity and morphology and dissolution enhancement has been studied using the poorly water soluble drug, naproxen. The NFs were prepared via wet milling using a conventional Retsch Planetary ball mill in various ratios of drug to polymer (1:1, 1:2, 1:3, 1:4). The release rate of naproxen from various ratios of drug/polymer nanoparticles was investigated using USP paddle apparatus (type II). A comparative phase solubility of naproxen was performed in different carrier concentrations of simulated gastric fluid (pH 1.2) and simulated intestinal fluid (pH 6.8). The highest dissolution enhancement was achieved for the formulation with ratio of 1:4. This is a 160% enhancement when compared to that of the pure drug. The ability of amphiphillic surfactant carriers to accelerate in vitro dissolution of poorly water-soluble drugs has been attributed to wetting, micellar solubilization, and/or deflocculation. The Korsemeyer–Peppas model most aptly fits the in vitro dissolution data and gives an insight into the possible drug release mechanisms predominated by anamolous non-Fickian diffusion. Thus, the nanoformulations studied can help improve the physicochemical characteristics of naproxen towards its dissolution enhancement and possibly will increase the oral bioavailability of the drug without any adverse cytotoxic consequences.},
 year = {2017}
}

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TY  - JOUR
T1  - Naproxen-Gelucire Nanoformulations for Improved Solubility and Dissolution Rate of Poorly Water-Soluble Drug Naproxen
AU  - Sandeep Patnaik
AU  - Aditya Dileep Kurdekar
AU  - Lakshmi Adinarayana Avinash Chunduri
AU  - Chinnakoti Prathibha
AU  - Kamisetti Venkataramaniah
Y1  - 2017/11/23
PY  - 2017
N1  - https://doi.org/10.11648/j.jddmc.20170306.11
DO  - 10.11648/j.jddmc.20170306.11
T2  - Journal of Drug Design and Medicinal Chemistry
JF  - Journal of Drug Design and Medicinal Chemistry
JO  - Journal of Drug Design and Medicinal Chemistry
SP  - 77
EP  - 85
PB  - Science Publishing Group
SN  - 2472-3576
UR  - https://doi.org/10.11648/j.jddmc.20170306.11
AB  - Naproxen-Gelucire Nanoformulations (NFs) in terms of their phase solubility behavior, physico-chemical characteristics, cytotoxicity and morphology and dissolution enhancement has been studied using the poorly water soluble drug, naproxen. The NFs were prepared via wet milling using a conventional Retsch Planetary ball mill in various ratios of drug to polymer (1:1, 1:2, 1:3, 1:4). The release rate of naproxen from various ratios of drug/polymer nanoparticles was investigated using USP paddle apparatus (type II). A comparative phase solubility of naproxen was performed in different carrier concentrations of simulated gastric fluid (pH 1.2) and simulated intestinal fluid (pH 6.8). The highest dissolution enhancement was achieved for the formulation with ratio of 1:4. This is a 160% enhancement when compared to that of the pure drug. The ability of amphiphillic surfactant carriers to accelerate in vitro dissolution of poorly water-soluble drugs has been attributed to wetting, micellar solubilization, and/or deflocculation. The Korsemeyer–Peppas model most aptly fits the in vitro dissolution data and gives an insight into the possible drug release mechanisms predominated by anamolous non-Fickian diffusion. Thus, the nanoformulations studied can help improve the physicochemical characteristics of naproxen towards its dissolution enhancement and possibly will increase the oral bioavailability of the drug without any adverse cytotoxic consequences.
VL  - 3
IS  - 6
ER  -

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Author Information

Sandeep Patnaik

Andhra Pradesh Medtech Zone, Vishakhapatnam, India
Aditya Dileep Kurdekar

Laboratories for Nanoscience and Nanotechnology Research, Department of Physics, Sri Sathya Sai Institute of Higher Learning, Prasanthinilayam, India
Lakshmi Adinarayana Avinash Chunduri

Andhra Pradesh Medtech Zone, Vishakhapatnam, India
Chinnakoti Prathibha

Laboratories for Nanoscience and Nanotechnology Research, Department of Physics, Sri Sathya Sai Institute of Higher Learning, Prasanthinilayam, India
Kamisetti Venkataramaniah

Laboratories for Nanoscience and Nanotechnology Research, Department of Physics, Sri Sathya Sai Institute of Higher Learning, Prasanthinilayam, India

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APA Style

Sandeep Patnaik, Aditya Dileep Kurdekar, Lakshmi Adinarayana Avinash Chunduri, Chinnakoti Prathibha, Kamisetti Venkataramaniah. (2017). Naproxen-Gelucire Nanoformulations for Improved Solubility and Dissolution Rate of Poorly Water-Soluble Drug Naproxen. Journal of Drug Design and Medicinal Chemistry, 3(6), 77-85. https://doi.org/10.11648/j.jddmc.20170306.11

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ACS Style

Sandeep Patnaik; Aditya Dileep Kurdekar; Lakshmi Adinarayana Avinash Chunduri; Chinnakoti Prathibha; Kamisetti Venkataramaniah. Naproxen-Gelucire Nanoformulations for Improved Solubility and Dissolution Rate of Poorly Water-Soluble Drug Naproxen. J. Drug Des. Med. Chem. 2017, 3(6), 77-85. doi: 10.11648/j.jddmc.20170306.11

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AMA Style

Sandeep Patnaik, Aditya Dileep Kurdekar, Lakshmi Adinarayana Avinash Chunduri, Chinnakoti Prathibha, Kamisetti Venkataramaniah. Naproxen-Gelucire Nanoformulations for Improved Solubility and Dissolution Rate of Poorly Water-Soluble Drug Naproxen. J Drug Des Med Chem. 2017;3(6):77-85. doi: 10.11648/j.jddmc.20170306.11

Copy | Download

@article{10.11648/j.jddmc.20170306.11,
  author = {Sandeep Patnaik and Aditya Dileep Kurdekar and Lakshmi Adinarayana Avinash Chunduri and Chinnakoti Prathibha and Kamisetti Venkataramaniah},
  title = {Naproxen-Gelucire Nanoformulations for Improved Solubility and Dissolution Rate of Poorly Water-Soluble Drug Naproxen},
  journal = {Journal of Drug Design and Medicinal Chemistry},
  volume = {3},
  number = {6},
  pages = {77-85},
  doi = {10.11648/j.jddmc.20170306.11},
  url = {https://doi.org/10.11648/j.jddmc.20170306.11},
  eprint = {https://article.sciencepublishinggroup.com/pdf/10.11648.j.jddmc.20170306.11},
  abstract = {Naproxen-Gelucire Nanoformulations (NFs) in terms of their phase solubility behavior, physico-chemical characteristics, cytotoxicity and morphology and dissolution enhancement has been studied using the poorly water soluble drug, naproxen. The NFs were prepared via wet milling using a conventional Retsch Planetary ball mill in various ratios of drug to polymer (1:1, 1:2, 1:3, 1:4). The release rate of naproxen from various ratios of drug/polymer nanoparticles was investigated using USP paddle apparatus (type II). A comparative phase solubility of naproxen was performed in different carrier concentrations of simulated gastric fluid (pH 1.2) and simulated intestinal fluid (pH 6.8). The highest dissolution enhancement was achieved for the formulation with ratio of 1:4. This is a 160% enhancement when compared to that of the pure drug. The ability of amphiphillic surfactant carriers to accelerate in vitro dissolution of poorly water-soluble drugs has been attributed to wetting, micellar solubilization, and/or deflocculation. The Korsemeyer–Peppas model most aptly fits the in vitro dissolution data and gives an insight into the possible drug release mechanisms predominated by anamolous non-Fickian diffusion. Thus, the nanoformulations studied can help improve the physicochemical characteristics of naproxen towards its dissolution enhancement and possibly will increase the oral bioavailability of the drug without any adverse cytotoxic consequences.},
 year = {2017}
}

Copy | Download

TY  - JOUR
T1  - Naproxen-Gelucire Nanoformulations for Improved Solubility and Dissolution Rate of Poorly Water-Soluble Drug Naproxen
AU  - Sandeep Patnaik
AU  - Aditya Dileep Kurdekar
AU  - Lakshmi Adinarayana Avinash Chunduri
AU  - Chinnakoti Prathibha
AU  - Kamisetti Venkataramaniah
Y1  - 2017/11/23
PY  - 2017
N1  - https://doi.org/10.11648/j.jddmc.20170306.11
DO  - 10.11648/j.jddmc.20170306.11
T2  - Journal of Drug Design and Medicinal Chemistry
JF  - Journal of Drug Design and Medicinal Chemistry
JO  - Journal of Drug Design and Medicinal Chemistry
SP  - 77
EP  - 85
PB  - Science Publishing Group
SN  - 2472-3576
UR  - https://doi.org/10.11648/j.jddmc.20170306.11
AB  - Naproxen-Gelucire Nanoformulations (NFs) in terms of their phase solubility behavior, physico-chemical characteristics, cytotoxicity and morphology and dissolution enhancement has been studied using the poorly water soluble drug, naproxen. The NFs were prepared via wet milling using a conventional Retsch Planetary ball mill in various ratios of drug to polymer (1:1, 1:2, 1:3, 1:4). The release rate of naproxen from various ratios of drug/polymer nanoparticles was investigated using USP paddle apparatus (type II). A comparative phase solubility of naproxen was performed in different carrier concentrations of simulated gastric fluid (pH 1.2) and simulated intestinal fluid (pH 6.8). The highest dissolution enhancement was achieved for the formulation with ratio of 1:4. This is a 160% enhancement when compared to that of the pure drug. The ability of amphiphillic surfactant carriers to accelerate in vitro dissolution of poorly water-soluble drugs has been attributed to wetting, micellar solubilization, and/or deflocculation. The Korsemeyer–Peppas model most aptly fits the in vitro dissolution data and gives an insight into the possible drug release mechanisms predominated by anamolous non-Fickian diffusion. Thus, the nanoformulations studied can help improve the physicochemical characteristics of naproxen towards its dissolution enhancement and possibly will increase the oral bioavailability of the drug without any adverse cytotoxic consequences.
VL  - 3
IS  - 6
ER  -

Copy | Download