Factors affecting preparation and evaluation of Kitorolac tromethamine microsponges for ocular use

Authors

  • Wid F. Neamah Ministry of health, Al-Karkh Health Department, Central Child Hospital
  • Nidhal K. Maraie Department of Pharmaceutics, College of Pharmacy, Mustansiriyah University, Baghdad, Iraq

DOI:

https://doi.org/10.32947/ajps.v20i3.761

Keywords:

: Microsponges, Ketorolac Tromethamine, poly lactic-co-glycolic acid (PLGA), poly vinyl alcohol (PVA).

Abstract

Ketorolac Tromethamine (KT) is prepared for the first time by double emulsion procedure. The current research involves preparation and evaluation of microsponges for ocular applications. This work included preparation of sixteen formulas of KT-microsponges by double

emulsion (w/o/w) method using poly lactic-co-glycolic acid (PLGA) as a polymer and poly vinyl alcohol (PVA) as a stabilizer, with different mixer types for different time and power. The prepared microsponges were characterized by Scanning Electron Microscopy (SEM) to investigate the morphology and particle size, the entrapment efficacy and percentage yield were calculated as well as in vitro drug release. Best formula (F14) of KT-microsponges had EE (74%), % yield (83%) with initial drug release (approximately 21% within the first fifteen days) which continued to reach (approximately 86% within 90 days) by using 30% of  PLGA  concentration with 0.05% of PVA and 200 ml of the external aqueous phase using a probe sonicator for 4 minutes at 200 Watt power. This formulation technique will be the interest of pharmaceutical company.

References

- Mandava SS, Thavva V. Novel approach: microsponge drug delivery system. International Journal of Pharmaceutical Sciences and Research. 2012 Apr 1;3(4):967-980.

- Srivastava R, Pathak K. Microsponges: a futuristic approach for oral drug delivery. Expert Opinion on Drug Delivery. 2012;9(7):863-78.

- Badhe KP, Saudagar RB. A Review on Microsponge a Novel Drug Delivery System. Asian Journal of Pharmaceutical Research. 2016;6(1):51-7.

- Wadhwa A, Mathura V, Lewis S. Emerging novel nanopharmaceuticals for drug delivery. Asian J Pharm Clin Res. 2018;11(7):35-42.

- Mohanty D, Bakshi V, Rashaid MA, Reddy TV, Dholakia NA, Babu AM. Design and in-vitro characterization of betamethasone microsponge loaded topical gel. International Journal of Pharma Research and Health Sciences Volume. 2016;4(2):1124-9.

- Shukla A, Garg A, Garg S. Application of microsponge technique in topical drug delivery system. Asian Journal of Biomaterial Research. 2016;2(4):120-126.

- Obiedallah MM, Abdel-Mageed AM, Elfaham TH. Ocular administration of acetazolamide microsponges in situ gel formulations. Saudi Pharmaceutical Journal. 2018;26(7):909-20.

- Handley DA, Cervoni P, McCray JE, McCullough JR. Preclinical Enantioselective Pharmacology of (R)‐and (S)‐Ketorolac. The Journal of Clinical Pharmacology. 1998;38:25-35.

- British pharmacopoeia, 2011; 1: 654-656.

- Uddin MN. A novel validated UPLC method for the estimation of ketorolac tromethamine in pharmaceutical formulation. Research. 2014; 1:1237-1248.

- Patil VP, Devdhe SJ, Angadi SS, Kale SH, Phalke SD, Shelke SD, Patil RH. Validated Spectrophotometric Method for the Estimation of Ketorolac Tromithamine in Bulk and Tablets Using Ninhydrin: A Modified Approach. Asian Journal of Research in Chemistry. 2014; 7(1):19-24.

- Pistel KF, Breitenbach A, Zange-Volland R, Kissel T. Brush-like branched biodegradable polyesters, part III: Protein release from microspheres of poly (vinyl alcohol)-graft-poly (D, L-lactic-co-glycolic acid). Journal of controlled release. 2001;73(1):7-20.

- Bhaskaran S, Suresh S. Biodegradable microspheres of ketorolac tromethamine for parenteral administration. Journal of microencapsulation. 2004;21(7):743-50.

- Mathew ST, Devi SG, Sandhya KV. Formulation and evaluation of ketorolac tromethamine-loaded albumin microspheres for potential intramuscular administration. Aaps Pharmscitech. 2007;8(1):1-9.

- Ng SF, Rouse J, Sanderson D, Eccleston G. A comparative study of transmembrane diffusion and permeation of ibuprofen across synthetic membranes using Franz diffusion cells. Pharmaceutics. 2010;2(2):209-230.

- Silva AF, Alves MA, Oliveira MS. Rheological behaviour of vitreous humour. Rheologica Acta. 2017;56(4):377-386.

- Swaminathan S, Vavia PR, Trotta F, Cavalli R. Nanosponges encapsulating dexamethasone for ocular delivery: formulation design, physicochemical characterization, safety and corneal permeability assessment. Journal of biomedical nanotechnology. 2013;9(6):998-1007.

- Raina B, Sharma A, Bajwa PS. Formulation evaluation and optimization of fast disintegrating tablets of ketorolac tromethamine. Jornal of Pharmaceutical Investigation . 2018;48(6):685–695.

- Kamble RS, Kajale AD, Bakade KP, Channawar MA, Chandewar AV. Formulation and development of enteric coated dosage form using ketorolac tromethamine. International Journal of Pharmaceutical Research and Development. 2010;2(8):126-135.

- Devarajan PV, Gore SP, Chavan SV. HPTLC determination of ketorolac tromethamine. Journal of pharmaceutical and biomedical analysis. 2000;22(4):679-683.

- Kumar J, Muralidharan S. Development of Microparticle Loaded Gel ( MPLGs ) for Prolong Ocular Drug Delivery Containing Ketorolac Tromethamine. Journal of pharmaceutical science and research. 2014;6(3):148–52.

- Mathew ST, Devi SG, Kv S. Formulation and Evaluation of Ketorolac Tromethamine-loaded Albumin Microspheres for Potential Intramuscular Administration. AAPS Pharmaceutics of Science and Technology . 2007;8(1):1-9.

- Jalil R, Nixon JR. Biodegradable poly(lactic acid) and poly(lactide-co-glycolide) microcapsules: Problems associated with preparative techniques and release properties. Journal of Microencapsulation. 1990;7(3):297–325.

- Leong TS, Martin GJ, Ashokkumar M. Ultrasonic encapsulation–a review. Ultrasonics sonochemistry. 2017;35:605-614.

- Bhatt P, Lalani R, Vhora I, Patil S, Amrutiya J, Misra A. Liposomes encapsulating native and cyclodextrin enclosed paclitaxel: Enhanced loading efficiency and its pharmacokinetic evaluation. International Journal of Pharmaceutics. 2018;536(1):95–107.

- Cohen S, Yoshioka T, Lucarelli M, Hwang LH, Langer R. Controlled delivery systems for proteins based on poly (lactic/glycolic acid) microspheres. Pharmaceutical research. 1991;8(6):713-720.

- Bilati U, Allémann E, Doelker E. Sonication parameters for the preparation of biodegradable nanocapsules of controlled size by the double emulsion method. Pharmaceutical development and technology. 2003;8(1):1-9.

- Manchanda R, Fernandez-fernandez A, Nagesetti A, Mcgoron AJ. Preparation and characterization of a polymeric ( PLGA ) nanoparticulate drug delivery system with simultaneous incorporation of chemotherapeutic and thermo-optical agents. Colloids and Surfaces B : Biointerfaces. 2010;75:260–267.

- Song X, Zhao Y, Hou S, Xu F, Zhao R. Dual agents loaded PLGA nanoparticles : Systematic study of particle size and drug entrapment efficiency. Sience Direct. 2008;69:445–453.

- Lee J, Gwan T, Choi H. Effect of formulation and processing variables on the characteristics of microspheres for water-soluble drugs prepared by w / o / o double emulsion solvent diffusion method. International Journal of Pharmaceutics. 2000;196:75–83.

- Gharehbeglou P, Jafari SM, Homayouni A, Hamishekar H, Mirzaei H. Fabrication of double W1/O/W2 nano-emulsions loaded with oleuropein in the internal phase (W1) and evaluation of their release rate. Food Hydrocolliods. 2018;10(20):1-6.

- Meng FT, Ma GH, Qiu W, Su ZG. W / O / W double emulsion technique using ethyl acetate as organic solvent : effects of its diffusion rate on the characteristics of microparticles. Journal of Controlled Release. 2003;91:407–416.

- Yang Y, Chung T, Ng NP. Morphology, drug distribution, and in vitro release profiles of biodegradable polymeric microspheres containing protein fabricated by double-emulsion solvent extraction/evaporation method. Biomaterials. 2001;22:231-241.

- Seju U, Kumar A, Sawant KK. Development and evaluation of olanzapine-loaded PLGA nanoparticles for nose-to-brain delivery : In vitro and in vivo studies. Acta Biomaterialia. 2011;7(12):4169–4176.

- Gizawy E, Sanaa A, Paul A. Effect of process variables on formulation, in-vitro characterisation and subcutaneous delivery of insulin PLGA nanoparticles: An optimisation study. Journal of Drug Delivery Science and Technology. 2018;43:160-171.

- Chen L, Mei L, Feng D, Huang D, Tong X, Pan X, Zhu C, Wu C. Anhydrous reverse micelle lecithin nanoparticles/PLGA composite microspheres for long-term protein delivery with reduced initial burst. Colloids and Surfaces B: Biointerfaces. 2018;163:146-54.

- Budhian A, Siegel SJ, Winey KI. Controlling the in vitro release profiles for a system of haloperidol-loaded PLGA nanoparticles. International Journal of Pharmaceutics. 2008 ;346(1-2):151-159.

- Ibrahim MM, Abd-elgawad AH, Soliman OA, Jablonski M. Nanoparticle-Based Topical Ophthalmic Formulations for Sustained Celecoxib Release. PharmaceuticalNanotechnology. 2013;102(3):1036–1053.

- Allison SD. Analysis of initial burst in PLGA microparticles. Informa Healthcare. 2008;5(6):615–628.

- Sun SW, Jeong YI, Jung SW, Kim SH. Characterization of FITC-albumin encapsulated poly (dl-lactide-co-glycolide) microspheres and its release characteristics. Journal of microencapsulation. 2003;20(4):479-488.

Downloads

Published

2020-09-01