Design of Salbutamol Sulphate Gastroretentive Nanoparticles via Surface Charge Manipulation
In the present study, development of salbutamol
sulphate nanoparticles that adhere to gastric mucus was investigated.
Salbutamol sulphate has low bioavailability due to short transit time in
gastric. It also has a positive surface charge that provides hurdles to be
encapsulated by the positively strong mucoadhesive polymer of
chitosan. To overcome the difficulties, the surface charge of active
ingredient was modified using several nonionic and anionic
stomach-specific polymers. The nanoparticles were prepared using
ionotropic gelation technique. The evaluation involved determination
of particle size, zeta potential, entrapment efficiency, in vitro drug
release and in vitro mucoadhesion test. Results exhibited that the use
of anionic alginate polymer was more satisfactory than that of
nonionic polymer. Characteristics of the particles was nano-size, high
encapsulation efficiency, fulfilled the drug release requirements and
adhesive towards stomach for around 11 hours. This result shows that
the salbutamol sulphate nanoparticles can be utilized for improvement
its delivery.
[1] S.K. Lai, Y. Wang, and J. Hanes, "Mucus-penetrating nanoparticles for
drug and gene delivery to mucosal tissues", Adv. Drug Deliv. Rev., vol.
61, no. 2, 2009, pp. 158-171.
[2] K. Sailaja, P. Amareshwar, and P. Chakravarty, "Chitosan nanoparticles
as a drug delivery systems", Res. J. Pharm. Biol. Chem. Sci., vol. 1, no. 3,
2010, pp. 474-484.
[3] W.H. Huang, Z.J. Yang, H. Wu, Y.F. Wong, Z.Z. Zhao, and L. Liu,"
Development of liposomal salbutamol sulphate dry powder inhaler
formulation", Biol. Pharm. Bull., vol. 33, no. 3, 2010, p. 527-517.
[4] E.S. El-Leithy, D.S. Shaker, M.K. Ghorab, and R.S. Abdel-Rashid,
"Evaluation of mucoadhesive hydrogels loaded with diclofenac
sodium-chitosan microspheres for rectal administration", AAPS Pharm.
Sci. Tech., vol. 11, no. 4, 2010, pp. 1695-1702.
[5] B. Patel, P. Patel, A. Bhosale, S. Hardikar, S. Mutha, and G. Chaulang,
"Evaluation of tamarind seed polysaccharide (TSP) as a mucoadhesive
and sustained release component of nifedipine buccoadhesive tablet &
comparison with HPMC and CMC Na", Int. J. Pharm. Tech. Res., vol. 1,
no. 3, 2009, pp. 404-410.
[6] C.R. Palem, R. Gannu, N. Doodipala, V.V. Yamsani, and M.R. Yamsani,
"Transmucosal delivery of domperidone from bilayered buccal patches:
in vitro, ex vivo and in vivo characterization", Arch. Pharm. Res., vol. 34,
no. 10, 2011, pp. 1701-1710.
[7] L. Bromberg, M. Temchenko, V. Alakhov, T.A. Hatton, "Bioadhesive
properties and rheology of polyether-modified poly(acrylic acid)
hydrogels", Int. J. Pharm., vol. 282, no. 1-2, 2004, pp. 45-60.
[8] S. Dhawan, V.R. Sinha, A.K. Singla, S. Wardhawan, R. Kaushik, R.
Kumria, and K. Bansal, "Chitosan microsphere as a potential carrier for
drugs", Int. J. Pharm., vol.274, 2004, pp. 1-33.
[9] P. Calvo, C. Remunan-Lopez, J.L. Vila-Jato, and M.J. Alonso, "Novel
hydrophilic chitosan-polyethylene oxide nanoparticles as protein
carriers", J. App. Pol. Sci, vol. 63, 1997, pp. 125-132.
[10] A. Nasti, N.M. Zaki, P. Leonardis, S. Ungphaiboon, P. Sansongsak, M.G.
Rimoli, and N. Tirelli, "Chitosan/TPP and Chitosan/TPP-hyaluronic acid
nanoparticles: systemic optimization of preparative process and
preliminary biological evaluation", Pharm. Res., vol. 26, no. 8, 2009, pp.
1918-1930.
[11] M.P. Deacon, S. McGurk, C.J. Roberts, P.M. William, S.J. Tendler, M.C.
Davies, S.S. Davis, and S.E. Harding,"Atomic force microscopy of
gastric mucin and chitosan mucoadhesive systems", Biochem. J., vol.
348, no. 3, 2000, pp. 557-563.
[12] T. Gazori, M.R. Khoshayand, E. Azizi, P. Yazdizade, A. Nomani, and I.
Haririan, "Evaluation of alginate/chitosan nanoparticles as antisense
delivery vector: formulation, optimization and in vitro characterization",
Carbohydrate Pol., vol 77, 2009, pp. 599-606.
[13] F.A. Oyarzun-Ampuero, J. Brea, M.I. Loza, D. Torres, and M.J. Alonso,
"Chitosan-hyaluronic acid nanoparticles loaded with heparin for
treatment of asthma", Int. J. Pharm., vol 381, 2009, pp. 122-129.
[14] S.B. Kiran, R.S. Dhumal, B. Chauhan, A. Paradkar, and S.S. Kadam,
"Effect of oppositely charged polymer and dissolution medium on
swelling, erosion, and drug release from chitosan matrices", AAPS
Pharm. Sci. Tech., vol. 8, no. 2, 2007, article 44.
[15] S.T. Lim, G.P. Martin, D.J. Berry, and M.B. Brown, "Preparation and
evaluation of the in vitro drug release properties and mucoadhesion of
novel microspheres of hyaluronic acid and chitosan", J. Control Rel., vol.
66, 2000, pp. 281-292.
[16] E. Rytting, M. Bur, R. Cartier, T. Bouyssou, X. Wang, M. Kruger, C.
Lehr, and T. Kissel, "In vitro and in vivo performance of biocompatible
negatively-charged salbutamol-loaded nanoparticles, J. Control Rel., vol.
141, 2010, pp. 101-107.
[17] U.V. Bannakar, Pharmaceutical Dissolution Testing, Marcell Dekker,
Inc., USA, 1992, pp. 322.
[1] S.K. Lai, Y. Wang, and J. Hanes, "Mucus-penetrating nanoparticles for
drug and gene delivery to mucosal tissues", Adv. Drug Deliv. Rev., vol.
61, no. 2, 2009, pp. 158-171.
[2] K. Sailaja, P. Amareshwar, and P. Chakravarty, "Chitosan nanoparticles
as a drug delivery systems", Res. J. Pharm. Biol. Chem. Sci., vol. 1, no. 3,
2010, pp. 474-484.
[3] W.H. Huang, Z.J. Yang, H. Wu, Y.F. Wong, Z.Z. Zhao, and L. Liu,"
Development of liposomal salbutamol sulphate dry powder inhaler
formulation", Biol. Pharm. Bull., vol. 33, no. 3, 2010, p. 527-517.
[4] E.S. El-Leithy, D.S. Shaker, M.K. Ghorab, and R.S. Abdel-Rashid,
"Evaluation of mucoadhesive hydrogels loaded with diclofenac
sodium-chitosan microspheres for rectal administration", AAPS Pharm.
Sci. Tech., vol. 11, no. 4, 2010, pp. 1695-1702.
[5] B. Patel, P. Patel, A. Bhosale, S. Hardikar, S. Mutha, and G. Chaulang,
"Evaluation of tamarind seed polysaccharide (TSP) as a mucoadhesive
and sustained release component of nifedipine buccoadhesive tablet &
comparison with HPMC and CMC Na", Int. J. Pharm. Tech. Res., vol. 1,
no. 3, 2009, pp. 404-410.
[6] C.R. Palem, R. Gannu, N. Doodipala, V.V. Yamsani, and M.R. Yamsani,
"Transmucosal delivery of domperidone from bilayered buccal patches:
in vitro, ex vivo and in vivo characterization", Arch. Pharm. Res., vol. 34,
no. 10, 2011, pp. 1701-1710.
[7] L. Bromberg, M. Temchenko, V. Alakhov, T.A. Hatton, "Bioadhesive
properties and rheology of polyether-modified poly(acrylic acid)
hydrogels", Int. J. Pharm., vol. 282, no. 1-2, 2004, pp. 45-60.
[8] S. Dhawan, V.R. Sinha, A.K. Singla, S. Wardhawan, R. Kaushik, R.
Kumria, and K. Bansal, "Chitosan microsphere as a potential carrier for
drugs", Int. J. Pharm., vol.274, 2004, pp. 1-33.
[9] P. Calvo, C. Remunan-Lopez, J.L. Vila-Jato, and M.J. Alonso, "Novel
hydrophilic chitosan-polyethylene oxide nanoparticles as protein
carriers", J. App. Pol. Sci, vol. 63, 1997, pp. 125-132.
[10] A. Nasti, N.M. Zaki, P. Leonardis, S. Ungphaiboon, P. Sansongsak, M.G.
Rimoli, and N. Tirelli, "Chitosan/TPP and Chitosan/TPP-hyaluronic acid
nanoparticles: systemic optimization of preparative process and
preliminary biological evaluation", Pharm. Res., vol. 26, no. 8, 2009, pp.
1918-1930.
[11] M.P. Deacon, S. McGurk, C.J. Roberts, P.M. William, S.J. Tendler, M.C.
Davies, S.S. Davis, and S.E. Harding,"Atomic force microscopy of
gastric mucin and chitosan mucoadhesive systems", Biochem. J., vol.
348, no. 3, 2000, pp. 557-563.
[12] T. Gazori, M.R. Khoshayand, E. Azizi, P. Yazdizade, A. Nomani, and I.
Haririan, "Evaluation of alginate/chitosan nanoparticles as antisense
delivery vector: formulation, optimization and in vitro characterization",
Carbohydrate Pol., vol 77, 2009, pp. 599-606.
[13] F.A. Oyarzun-Ampuero, J. Brea, M.I. Loza, D. Torres, and M.J. Alonso,
"Chitosan-hyaluronic acid nanoparticles loaded with heparin for
treatment of asthma", Int. J. Pharm., vol 381, 2009, pp. 122-129.
[14] S.B. Kiran, R.S. Dhumal, B. Chauhan, A. Paradkar, and S.S. Kadam,
"Effect of oppositely charged polymer and dissolution medium on
swelling, erosion, and drug release from chitosan matrices", AAPS
Pharm. Sci. Tech., vol. 8, no. 2, 2007, article 44.
[15] S.T. Lim, G.P. Martin, D.J. Berry, and M.B. Brown, "Preparation and
evaluation of the in vitro drug release properties and mucoadhesion of
novel microspheres of hyaluronic acid and chitosan", J. Control Rel., vol.
66, 2000, pp. 281-292.
[16] E. Rytting, M. Bur, R. Cartier, T. Bouyssou, X. Wang, M. Kruger, C.
Lehr, and T. Kissel, "In vitro and in vivo performance of biocompatible
negatively-charged salbutamol-loaded nanoparticles, J. Control Rel., vol.
141, 2010, pp. 101-107.
[17] U.V. Bannakar, Pharmaceutical Dissolution Testing, Marcell Dekker,
Inc., USA, 1992, pp. 322.
@article{"International Journal of Medical, Medicine and Health Sciences:58266", author = "Diky Mudhakir and M. Fauzi Bostanudin and Fiki Firmawan and Rachmat Mauludin", title = "Design of Salbutamol Sulphate Gastroretentive Nanoparticles via Surface Charge Manipulation", abstract = "In the present study, development of salbutamol
sulphate nanoparticles that adhere to gastric mucus was investigated.
Salbutamol sulphate has low bioavailability due to short transit time in
gastric. It also has a positive surface charge that provides hurdles to be
encapsulated by the positively strong mucoadhesive polymer of
chitosan. To overcome the difficulties, the surface charge of active
ingredient was modified using several nonionic and anionic
stomach-specific polymers. The nanoparticles were prepared using
ionotropic gelation technique. The evaluation involved determination
of particle size, zeta potential, entrapment efficiency, in vitro drug
release and in vitro mucoadhesion test. Results exhibited that the use
of anionic alginate polymer was more satisfactory than that of
nonionic polymer. Characteristics of the particles was nano-size, high
encapsulation efficiency, fulfilled the drug release requirements and
adhesive towards stomach for around 11 hours. This result shows that
the salbutamol sulphate nanoparticles can be utilized for improvement
its delivery.", keywords = "Mucoadhesive, salbutamol sulphate, nanosize,
anionic polymer.", volume = "6", number = "12", pages = "681-7", }