TOPICAL GEL INCORPORATED WITH NON-IONIC SURFACTANT BASED SOLID LIPID MICROSPHERES OF KETOPROFEN: PHYSICOCHEMICAL ANALYSIS AND ANTI-INFLAMMATORY EVALUATION

Authors

  • Rashmi Sareen Shoolini University Bharat Institution of Technology
  • Varun Bhardwaj Jaypee University of Information Technology
  • Vineet Mehta Kurukshetra University
  • Arun Sharma Shoolini University Jaypee University of Information Technology

Keywords:

Ketoprofen, Solid lipid microsphere, Controlled release, Anti-inflammatory activity

Abstract

Objective: The present study was aimed at the fabrication and characterization of solid lipid based microspheres (SLM) of Ketoprofen (KPF) and comparing its anti-inflammatory potential with the marketed formulation.

Methods: Stearic acid as a lipid and tween 20, 80, span 20 and 80 as surfactants (at various concentrations) were utilized for formulation of topical delivery. Microparticles were successfully fabricated (0.71-3.12 µm) by hot melt microencapsulation technique and were characterised by photomicroscope, FTIR, scanning electron surface morphology, particle size analysis, zeta potential, fluorescent microscopy and In-vitro drug release studies followed by In-vitro and In-vivo anti-inflammatory studies.

Results: Results revealed that tween 80 resulted in exceptional KPF entrapment efficiency of 82.6% with spherical rough surface morphology. In-vitro drug release showed the initial burst release of 47% upto 2h followed by sustained release of 70% for 12h. By employing drug release kinetic modelling, formulations were found to obey Higuchi model and Korsmeyer-Peppas model. Further the In-vitro permeation study of optimized gel formulation represented better drug uptake through rat skin in comparison to marketed product. Finally, SLMs were found to possess superior In-vitro and In-vivo anti-inflammatory potentials when compared to marketed formulation.

Conclusion: SLMs proved to be promising drug carrier system for KPF topical delivery as they possessed the desirable particle size with high ability for drug entrapment with sustained anti-inflammatory effect.

 

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References

Hooshmand H, Hashmi M, Phillips EM. Infrared thermal imaging as a tool in pain management-An 11 Y Study, Part I of II. Thermol Int 2001;11:117-29.

Davis CC, Squier CA, Lilly GE. Irritant contact stomatitis: a review of the condition. J Periodontol 1998;69:620-31.

Buckwalter JA, Lappin DR. The disproportionate impact of chronic arthralgia and arthritis among women. Clin Orthop Relat Res 2000;372:159-68.

Fiorucci S, Meli R, Bucci M, Cirino G. Dual inhibitors of cyclooxygenase and 5-lipoxygenase. A new avenue in anti-inflammatory therapy? Biochem Pharmacol 2001;62:1433-8.

Hersh EV, Lally ET, Moore PA. Update on cyclooxygenase inhibitors: has a third COX isoform entered the fray. Curr Med Res Opin 2005;21:1217-26.

Gertz M, Harrison A, Houston JB, Galetin A. Prediction of human intestinal first-pass metabolism of 25 CYP3A substrates from in vitro clearance and permeability data. Drug Metab Dispos 2010;38:1147-58.

Oates JA, Wood AJ, Brooks PM, Day RO. Nonsteroidal antiinflammatory drugs—differences and similarities. N Engl J Med 1991;324:1716-25.

Kantor TG. Ketoprofen: a review of its pharmacologic and clinical properties. Pharmacotherapy: J Human Pharmacol Drug Ther 1986;6:93-102.

Small G, Dubois B. A review of compliance to treatment in Alzheimer's disease: potential benefits of a transdermal patch. Curr Med Res Opinion 2007;23:2705-13.

Prausnitz MR, Langer R. Transdermal drug delivery. Nat Biotechnol 2008;26:1261-8.

Capan Y, Jiang G, Giovagnoli S, Na K-H, DeLuca PP. Preparation and characterization of poly (D, L-lactide-co-glycolide) microspheres for controlled release of human growth hormone. AAPS PharmSciTech 2003;4:147-56.

Jaspart S, Piel G, Delattre L, Evrard B. Solid lipid microparticles: formulation, preparation, characterisation, drug release and applications. Expert Opin Drug Delivery 2005;2:75-87.

Almeida AJ, Souto E. Solid lipid nanoparticles as a drug delivery system for peptides and proteins. Adv Drug Delivery Rev 2007;59:478-90.

Audu MM, Achile PA, Amaechi AA. Phospholipon 90G based SLMs Loaded with Ibuprofen: an oral anti-inflammatory and gastrointestinal sparing evaluation in rats. Pak J Zool 2012;44:1657-64.

MuÈller RH, MaÈder K, Gohla S. Solid lipid nanoparticles (SLN) for controlled drug delivery–a review of the state of the art. Eur J Pharm Biopharm 2000;50:161-77.

Sanna V, Kirschvink N, Gustin P, Gavini E, Roland I, Delattre L, et al. Preparation and in vivo toxicity study of solid lipid microparticles as carrier for pulmonary administration. AAPS PharmSciTech 2004;5:17-23.

Gavini E, Sanna V, Sharma R, Juliano C, Usai M, Marchetti M, et al. Solid lipid microparticles (SLM) containing juniper oil as anti-acne topical carriers: preliminary studies. Pharm Dev Technol 2005;10:479-87.

López A, Llinares F, Cortell C, Herraez M. Comparative enhancer effects of Span® 20 with Tween® 20 and Azone® on the in vitro percutaneous penetration of compounds with different lipophilicities. Int J Pharm 2000;202:133-40.

Reithmeier H, Herrmann J, Göpferich A. Lipid microparticles as a parenteral controlled release device for peptides. J Controlled Release 2001;73:339-50.

Higuchi T. Mechanism of sustainedâ€action medication. Theoretical analysis of rate of release of solid drugs dispersed in solid matrices. J Pharm Sci 1963;52:1145-9.

Higuchi T. Rate of release of medicaments from ointment bases containing drugs in suspension. J Pharm Sci 1961;50:874-5.

Korsmeyer RW, Gurny R, Doelker E, Buri P, Peppas NA. Mechanisms of solute release from porous hydrophilic polymers. Int J Pharm 1983;15:25-35.

Sareen R, Kumar S, D Gupta G. Meloxicam carbopol-based gels: characterization and evaluation. Curr Drug Delivery 2011;8:407-15.

Patel D, Dasgupta S, Dey S, Ramani YR, Ray S, Mazumder B. Nanostructured lipid carriers (NLC)-based gel for the topical delivery of aceclofenac: preparation, characterization, and in vivo evaluation. Sci Pharm 2012;80:749.

Mizushima Y, Kobayashi M. Interaction of antiâ€inflammatory drugs with serum proteins, especially with some biologically active proteins. J Pharm Pharmacol 1968;20:169-73.

Asanuma M, Taguchi C, Kumagi T, Uesaka H, Hosokawa H, Kuriya S-i. The hydrogen ion concentration (pH) in blood samples with K2EDTA and K3EDTA affects mean corpuscular volume values in hemodialysis patients. Lab Hematol 2000;6:67-72.

Sadique J, Al-Rqobah W, Bughaith M, El-Gindy A. The bio-activity of certain medicinal plants on the stabilization of RBC membrane system. Fitoterapia 1989;60:525-32.

Gandhidasan R, Thamaraichelvan A, Baburaj S. Anti-inflammatory action of Lannea coromandelica by HRBC membrane stabilization. Fitoterapia 1991;62:81-3.

Nasr M, Mansour S, Mortada ND, El Shamy A. Lipospheres as carriers for topical delivery of aceclofenac: preparation, characterization and in vivo evaluation. AAPS PharmSciTech 2008;9:154-62.

Escribano E, Calpena AC, Queralt J, Obach R, Doménech J. Assessment of diclofenac permeation with different formulations: anti-inflammatory study of a selected formula. Eur J Pharm Sci 2003;19:203-10.

Paudel KS, Milewski M, Swadley CL, Brogden NK, Ghosh P, Stinchcomb AL. Challenges and opportunities in dermal/transdermal delivery. Ther Delivery 2010;1:109-31.

Mei Z, Chen H, Weng T, Yang Y, Yang X. Solid lipid nanoparticle and microemulsion for topical delivery of triptolide. Eur J Pharm Biopharm 2003;56:189-96.

Published

01-10-2015

How to Cite

Sareen, R., V. Bhardwaj, V. Mehta, and A. Sharma. “TOPICAL GEL INCORPORATED WITH NON-IONIC SURFACTANT BASED SOLID LIPID MICROSPHERES OF KETOPROFEN: PHYSICOCHEMICAL ANALYSIS AND ANTI-INFLAMMATORY EVALUATION”. International Journal of Pharmacy and Pharmaceutical Sciences, vol. 7, no. 11, Oct. 2015, pp. 199-06, https://journals.innovareacademics.in/index.php/ijpps/article/view/7532.

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Original Article(s)