DEVELOPMENT OF STABLE NANOSUSPENSION LOADED ORAL FILMS OF GLIMEPIRIDE WITH IMPROVED BIOAVAILABILITY
DOI:
https://doi.org/10.22159/ijap.2017v9i2.16714Keywords:
Nanosuspension, Glimepiride, Stabilization, Solidification, In vivo studiesAbstract
Objective: In the present work attempt has been made to stabilize optimized nanosuspensions of glimepiride by solidification using a novel Oral Thin Film (OTF) formulation.
Methods: Nanosuspensions were characterized for particle size, zeta potential as well as in vitro dissolution profile. As nanosuspensions are prone to destabilization by Ostwald's ripening or agglomeration/aggregation, OTF formulation as a novel approach for stabilization through solidification of optimized nanosuspension was attempted. OTF formulation method is a simple, easy and scalable method for the preparation of solid oral dosage form. Prepared formulations were evaluated for physicochemical parameters like folding endurance, disintegration time, tensile strength, in vitro drug release, in vivo bioavailability and stability.
Results: The mean particle size of the nanoparticles in OTF was found to be 57.2 nm. It was observed from the results of in vivo bioavailability studies that high plasma drug concentrations(Cmax) were achieved for nanosuspension loaded OTF (NSOTF) i.e. 4900 ng/ml as compared to marketed oral formulation (Cmax-2900 ng/ml). Results of the stability studies indicated that nanosize of the particles was retained even after 3 mo of the study.
Conclusion: Therefore it can be concluded that OTF formulation has a potential for stabilization of nanosuspensions.
Downloads
References
Cooper ER. Nanoparticles: a personal experience for formulat-ing poorly water-soluble drugs. J Controlled Release 2010;141:300-2.
Wang Y, Zhang L, Wang Q, Zhang D. Stability issue of nanosus-pensions in drug delivery. J Controlled Release 2013;172:1126-41.
Laxmi P, Ashwinikumar G. Nanosuspension technology: a review. Int J Pharm Pharm Sci 2010;(2 Suppl 4):35-¬40.
Baek I, Kim J, Eun-Sol Ha, Gwang-Ho Choo. Dissolution and oral absorption of pranlukast nanosuspensions stabilized by hydroxypropylmethylcellulose. Int J Biol Macromol 2014;67:53-7.
Baumgartner R, Birgit J Teubl, Carolin Tetyczka, Roblegg E. Ratinal design and characterization of a nanosuspension for intraoral administration considering physiological conditions. J Pharm Sci 2016;105:257-67.
Singh SK, Srinivasan KK, Gowthamarajan K, Singare DS, Pra-kash D, Gaikwad NB. Investigation of preparation parameters of nanosuspension by top-down media milling to improve the dissolution of poorly water-soluble glyburide. Eur J Pharm Biopharm 2011;71:441-6.
Ghosh S, Bose R, Vippagunta F. Harmon. Nanosuspension for improving the bioavailability of a poorly soluble drug and screening of stabilizing agents to inhibit crystal growth. Int J Pharm 2011;409:260-8.
Rachmawati H, Al Shaal L, Muller RH, Keck CM. Development of curcumin nanocrystal: physical aspects. J Pharm Sci 2013;102;204-14.
He W, Lu Y, Qi J, Chen L, Hu F, Wu W. Food proteins as novel nanosuspension stabilizers for poorly water-soluble drugs. Int J Pharm 2013;441:269-78.
Gao YA, Qian SA, Zhang JJ. Physicochemical and pharmacoki-netic characterization of a spray-dried cefpodoxime proxetil nanosuspension. Chem Pharm Bull 2010;58:912-7.
Mezhericher M, Naumann M, Peglow M, Levy A, Tsotsas E, Borde I. Continuous species transport and population balance models for first drying stage of nanosuspension droplets. Chem Eng J 2012;210:120-35.
Eerdenbrugh VB, Froyen L, Humbeeck JV, Martens JA, Au-gustijns P, Mooter G. Drying of crystalline drug nanosuspen-sions–the importance of surface hydrophobicity on dissolu-tion behaviour upon redispersion. Eur J Pharm Sci 2008;35:127-35.
Gupta S, Samanta MK, Raichur AM. Dual-drug delivery system based on in situ gel-forming nanosuspension of forskolin to enhance antiglaucoma efficacy. AAPS PharmSciTech 2010;11:322-35.
Chonkar AD, Venkat Rao JRS, Managuli RS, S Mutalik. Develop-ment of fast dissolving oral films containing lercanidipine hcl nanoparticles in the semicrystalline polymeric matrix for en-hanced dissolution and ex vivo permeation. Eur J Pharm Bio-pharm 2016;103:179-91.
Steiner D, Finke JH, Kwade A. Efficient production of nanopar-ticle-loaded orodispersible films by process integration in a stirred media mill. Int J Pharm 2016;511:804-13.
Shen B, Shen C, Yuan X. Development and characterization of an orodispersible film containing drug nanoparticles. Eur J Pharm Biopharm 2013;85:1348-56.
Figueroaa L, Bhakaya A, Jackeline I, Rozob J. Preparation and characterization of hydroxypropyl methyl cellulose films con-taining stable BCS Class II drug nanoparticles for pharmaceu-tical applications. Int J Pharm 2012;423:496–508.
Bhanja SC, Shafeeque M, Sudhakar M. Mucoadhesive buccal tablets of glimepiride-formulation and evaluation. Int J Pharm Pharm Sci 2013;4:502-10.
Chaudhari MD, Sonawane RO, Zawar L, Nayak S, Bari SB. Solu-bility and dissolution enhancement of poorly water-soluble glimepiride by using solid dispersion technique. Int J Pharm Pharm Sci 2012;(4, Suppl 5):534-9.
Ammar HO, Salama HA, Ghorab M, Mahmoud AA. Formulation and biological evaluation of glimepiride–cyclodextrin–polymer systems. Int J Pharm 2006;309:129–38.
Nagpal M, Rajera R, Nagpal K, Rakha P, Singh S, Mishra D. Disso-lution enhancement of glimepiride using modified gum karaya as a carrier. Int J Pharm Investigation 2012;2:42-7.
Okonogi S, Puttipipatkhachorn S. Dissolution improvement of igh drug-loaded solid dispersion. AAPS PharmSciTech 2006;7:1–6.
Thakar D, Bharadia P, Pandya V. Enhancement of solubility of poorly water soluble antihypertensive drug by the nanosizing approach. J Pharm Bioall Sci 2012;4(Suppl 1):S40-S41.
Muhammad I, Sumeira R, Quratulain B. Orally disintegrating films: a modern expansion in drug delivery system. Saudi Pharm J 2016;24:537–46.
Esfandia E, Ramezania V, Vatanaraa A. Clarithromycin dissolu-tion enhancement by preparation of aqueous nanosuspen-sions using sonoprecipitation technique. Iranian J Pharma Res 2014;13:809-18.
Ghosh I, Bose S, Vippagunta R, Harmon F. Nanosuspension for improving the bioavailability of a poorly soluble drug and screening of stabilizing agents to inhibit crystal growth. Int J Pharm 2011;409:260-8.
Sievens-Figueroa L, Bhakay A, Jackeline I. Preparation and characterization of hydroxypropyl methyl cellulose films con-taining stable BCS Class II drug nanoparticles for pharmaceu-tical applications. Int J Pharm 2012;423:496–508.
Yokoi Y, Yonemochi E, Terada K. Effects of sugar ester and hydroxypropyl methylcellulose on the physicochemical sta-bility of amorphous cefditoren pivoxil in aqueous suspension. Int J Pharm 2005;290:91-9.
Published
How to Cite
Issue
Section
