DEVELOPMENT OF MUCOADHESIVE DELIVERY OF CHLORZOXAZONE POLYETHYLENE GLYCOL SOLID DISPERSION

Authors

  • Swati C Jagdale
  • Asawaree A Hable
  • Aniruddha R Chabukswar
  • Bhanudas S Kuchekar

Abstract

ABSTRACT
Objective: Chlorzoxazone (CLZ) is centrally acting skeletal muscle relaxant. It is insoluble in water, so employed for the formation of solid dispersions
(SD) as a means to enhance the dissolution rate, and carrier selected was polyethylene glycol 6000 (PEG 6000).
Methods: The SDs were prepared by different methods and characterized by in vitro drug release, drug content, fourier transform infrared
spectroscopy (FTIR), differential scanning calorimetry, powder X-ray diffraction. All the SD showed dissolution improvement compare to pure drug.
These techniques revealed distinct loss of drug crystallinity in the formulation accounting for enhancement in dissolution rate. The SD methods
showing best in vitro drug release profile were selected in the further development of mucoadhesive buccal patches. A buccal patch has been developed
using two mucoadhesive polymers, i.e. hydroxyl propyl methyl cellulose K4M and carbopol 974. The patches were evaluated for the physicochemical,
mechanical and drug release characteristics. The optimized patches showed good mechanical and physicochemical properties to withstand the
environment of the oral cavity. The in-vitro permeation study showed that patches could deliver drug to the oral mucosa for a period of 8 hrs.
Results: The results indicate that suitable bioadhesive buccal patches with good permeability could be prepared. The batches FH4 and FC4 showed
81.95% and 79.97% permeated through goat mucosa membrane in 8 hrs. The physicochemical interactions were investigated by FTIR, showed no
any evidence of interactions and were present in an unchanged state. The stability study for SD and buccal patch carried out revealed that were stable
for a period of 3-month.
Conclusion: Phase-solubility studies indicate significantly increase in solubility. The optimized buccal patches showed good mechanical and
physicochemical properties to withstand environment of the oral cavity.
Keywords: Solid dispersions, Chlorzoxazone, Dissolution studies, Buccal patch, In vitro permeation studies.

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References

REFERENCES

Dressman JB, Vertzoni M, Goumas K, Reppas C. Estimating

drug solubility in the gastrointestinal tract. Adv Drug Deliv Rev

;59(7):591-602.

Löbenberg R, Amidon GL. Modern bioavailability, bioequivalence

and biopharmaceutics classification system. New scientific approaches

to international regulatory standards. Eur J Pharm Biopharm

;50(1):3-12.

Zakeri-Milani P, Barzegar-Jalali M, Azimi M, Valizadeh H.

Biopharmaceutical classification of drugs using intrinsic dissolution

rate (IDR) and rat intestinal permeability. Eur J Pharm Biopharm

;73(1):102-6.

Guneri T, Taneri F, Ertan G. Studies on sustained release matrix systems

of chlorzoxazone. Acta Pharm Turcica 2005;47:39-51.

Reddy P. Simultaneous estimation of nimesulide and chlorzoxazone in

pharmaceutical formulations by a RP-HPLC method. Int J ChemTech

Res 2009;1(2):283-5.

Fawaz F, Bonini F, Guyot M, Bildet J, Maury M, Laguency AM.

Bioavailability of norfloxacin from PEG 6000 solid dispersion

and cyclodextrin inclusion complexes in rabbits. Int J Pharm

;132:271-5.

Van den Mooter G, Augustijns P, Blaton N, Kinget R. Physico-chemical

characterization of solid dispersions of temazepam with polyethylene

glycol 6000 and PVP K30. Int J Pharm 1998;164:67-80.

Leuner C, Dressman J. Improving drug solubility for oral delivery using

solid dispersions. Eur J Pharm Biopharm 2000;50(1):47-60.

Prajapati BG, Patel MM. Conventional and alternative pharmaceutical

methods to improve oral bioavailability of lipophilic drugs. Asian J

Pharm 2007;1(1):1-8.

Rao M, Mandag Y, Thanki K, Bhise S. Dissolution improvement of

simvastatin by surface solid dispersion technology. Dissolution Technol

;27:37-4.

Breitenbach J, Schrof W, Neumann J. Confocal Raman-spectroscopy:

Analytical approach to solid dispersions and mapping of drugs. Pharm

Res 1999;16(7):1109-13.

Amrutkar PP, Patil SB, Todarwal AN, Wagh MA, Kothawade PD,

Surawase RK. Design and evaluation of taste masked chewable

dispersible tablet of lamotrigine by melt granulation. Int J Drug Deliv

;2:183-91.

Shimpi S, Chauhan B, Mahadik KR, Paradkar A. Preparation and

evaluation of diltiazem hydrochloride-Gelucire 43/01 floating granules

prepared by melt granulation. AAPS PharmSciTech 2004;5(3):e43.

Patil S, Kuchekar B, Chabukswar A, Jagdale S. Formulation and

evaluation of extended-release solid dispersion of metformin

hydrochloride. J Young Pharm 2010;2(2):121-9.

Patel VM, Prajapati BG, Patel MM. Effect of hydrophilic polymers on

buccoadhesive Eudragit patches of propranolol hydrochloride using

factorial design. AAPS PharmSciTech 2007;8(2):Article 45.

Wong CF, Yuen KH, Peh KK. Formulation and evaluation

of controlled release Eudragit buccal patches. Int J Pharm

;178(1):11-22.

Nafee NA, Ismail FA, Boraie NA, Mortada LM. Mucoadhesive buccal

patches of miconazole nitrate: In vitro/in vivo performance and effect of

ageing. Int J Pharm 2003;264(1-2):1-14.

Peh KK, Wong CF. Polymeric films as vehicle for buccal delivery:

Swelling, mechanical, and bioadhesive properties. J Pharm Pharm Sci

;2(2):53-61.

Junginger HE, Hoogstraate JA, Verhoef JC. Recent advances in buccal

drug delivery and absorption – In vitro and in vivo studies. J Control

Release 1999;62(1-2):149-59.

Jagdale SC, Hable AA, Kuchekar BS, Chabukswar AR. Improvement

of dissolution rate of chlorzoxazone by solid dispersion technique

and development of buccal patch. J Appl Solut Chem Model

;2(2):145-57.

Jagdale SC, Mohanty P, Chabukswar AR, Kuchekar BS. Dissolution

rate enhancement, design and development of buccal drug delivery

of darifenacin hydroxypropyl ß-cyclodextrin inclusion complexes.

J Pharm (Cairo) 2013;2013:983702.

Published

01-03-2016

How to Cite

Jagdale, S. C., A. A. Hable, A. R. Chabukswar, and B. S. Kuchekar. “DEVELOPMENT OF MUCOADHESIVE DELIVERY OF CHLORZOXAZONE POLYETHYLENE GLYCOL SOLID DISPERSION”. Asian Journal of Pharmaceutical and Clinical Research, vol. 9, no. 2, Mar. 2016, pp. 145-9, https://mail.innovareacademics.in/journals/index.php/ajpcr/article/view/10166.

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