• RAJASHRI B. AMBIKAR PDEA’s Seth Govind Raghunath Sable College of Pharmacy, Saswad, Purandar, Pune, Maharashtra, India
  • ASHOK V. BHOSALE PDEA’s Shankarrao Ursal College of Pharmaceutical Sciences and Research Centre, Kharadi, Pune, Maharashtra, India



Microsponge, Ocular in situ gel, Controlled release, Ophthalmic drug delivery, Kinetic release


Objective: Purpose of the study to design and formulate Diclofenac sodium (DIC) microsponges.

Methods: With varied polymer: drug ratio DIC loaded microsponges were prepared with Eudragit RS100 polymer by quasi solvent diffusion method. Microsponges evaluated for particle size, entrapment efficiency, drug content, in vitro drug release, Fourier Transform Infrared Spectroscopy (FTIR), Differential scanning calorimetry (DSC) and Scanning electron microscopy (SEM). DIC loaded microsponges incorporated into ocular in situ gel to attained controlled release by microsponge and improved residence time by gelling system. Ocular in situ gel evaluated for pH, drug content determination, gelling capacity, in vitro drug release and sterility study.

Results: DSER4 microsponge formulation having polymer to drug ratio 1:7 showed satisfactory production yield (68.13%), entrapment efficiency (62.86%), drug content (80.73%), requisite particle size (less than 10 µm) (7.52 µm) and in vitro release 87.94% after 6 h. Selected DSER4 formulation was incorporate into in situ gel. Carbopol 940 forms stiff gel at higher pH so used as a gelling agent, whereas Hydroxypropyl Methylcellulose E4M was used as a viscosity-enhancing agent for the formulation of in situ gel in varied compositions. In situ gel formulation IG4 showed sustained release of 76.92% till the end of 8 h and satisfactory gelling capacity so IG4 further evaluated for sterility test. Rheological studies reveal the sol-gel transition of in situ gel occur at the physiological condition to form stiff gel.

Conclusion: Prepared in situ gel formulations showed sustained drug release for a period of 8 h, which is satisfactory for management of ocular pain.


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Osmani RA, Aloorkar NH, Kulkarni AS, Thaware BU, Kulkarni PK. Microsponge based drug delivery system for augmented gastroparesis therapy: formulation development and evaluation. Asian J Pharm Sci 2015;10:442-51.

Nokhodchi A, Jelvehgari M, Siahi MR, Mozafari MR. Factors affecting the morphology of benzoyl peroxide microsponges. Micron 2007;38:834–40.

Kumari A, Jain A, Hurkat P, Tiwari A, Jain SK. Eudragit S100 coated microsponges for Colon targeting of prednisolone. Drug Dev Ind Pharm 2018;44:902-13.

Sareen R, Nath K, Jain N, Dhar KL. Curcumin loaded microsponges for colon targeting in inflammatory bowel disease: fabrication, optimization, and in vitro and pharmacodynamic evaluation. J Biomed Biotechnol 2014. DOI:10.1155/2014/340701.

Srivastava R, Kumar D, Pathak K. Colonic luminal surface retentive Meloxi-cam microsponges delivered by erosion based colon targeted matrix tablet. Int J Pharm 2012;427:156–62.

Bhatia M, Saini M. Formulation and evaluation of curcumin microsponges for oral and topical drug delivery. Prog Biomater 2018;7:239–48.

Abdelmalak NS, El-Menshawe SF. A new topical fluconazole microsponge loaded hydrogel: preparation and characterization. Int J Pharm Pharm Sci 2012;4:460–9.

Arya P, Pathak K. Assessing the viability of microsponges as gastro retentive drug delivery system of curcumin: Optimization and pharmacokinetics. Int J Pharm 2014;460:1–12.

Maiti S, Kaity S, Ray S, Sa B. Development and evaluation of xanthan gum-facilitated ethyl cellulose microsponges for controlled percutaneous delivery of diclofenac sodium. Acta Pharm 2011;61:257–70.

Ambikar RB, Bhosale AV. Formulation and evaluation of eudragit Rl100 polymeric drug loaded microsponge for ophthalmic use. J Pharm Res Int 2021;33:45-51.

Abd-Elal RMA, Elosaily GH, Gad S. Full factorial design, optimization, in vitro and ex vivo studies of ocular timolol-loaded microsponges. J Pharm Innov 2020;15:651–63.

Obiedallah MM, Abdel-Mageed AM, Elfaham TH. Ocular administration of acetazolamide microsponges in situ gel formulations. Saudi Pharm J 2018;26:909–20.

Ali J, Fazil M, Qumbar M, Khan N, Ali A. Colloidal drug delivery system: amplify the ocular delivery. Drug Delivery 2016;23:710-26.

Kesarla R, Tank T, Vora PA, Shah T, Parmar S, Omri A. Preparation and evaluation of nanoparticles loaded ophthalmic in situ gel. Drug Delivery 2016;23:2363–70.

Upadhayay P, Kumar M, Pathak K. Norfloxacin loaded pH triggered nanoparticulate in-situ gel for extraocular bacterial infections: optimization, ocular irritancy and corneal toxicity. Iran J Pharm Sci 2016;15:3-22.

Al-Kinani A, Zidan G, Elsaid N, Seyfoddin A, Alani AW, Alany R. Ophthalmic gels: past, present and future. Adv Drug Delivery Rev 2018;126:113–26.

Wu Y, Liu Y, Li X, Kebebe D, Zhang B, Ren J, et al. Research progress of in-situ gelling ophthalmic drug delivery system. Asian J Pharm Sci 2019;14:1–15.

Khangtragool A. Methocel E4M: preparation and properties as a vehicle for the ocular drug delivery of vancomycin, Chiang Mai J Sci 2014;41:166-73.

Adelli GR, Balguri SP, Bhagav P, Raman V, Majumdar S. Diclofenac sodium ion exchange resin complex loaded melt cast films for sustained release ocular delivery. Drug Delivery 2017;24:370–9.

Jelvehgari M, Siahi Shadbad MR, Azarmi S, Martin GP, Nokhodchi A. The microsponge delivery system of benzoyl peroxide: preparation, characterization and release studies. Int J Pharm 2006;308:124–32.

Martin A, Bustamante P, Chun A. Micromeritics. In: Physical pharmacy–physical chemical principles in the pharmaceutical science. 5th ed. B I Waverly Pvt. Ltd; 2002. p. 446–8.

Nair AB, Shah J, Jacob S, Al-Dhubiab BE, Sreeharsha N. Experimental design, formulation and in vivo evaluation of a novel topical in situ gel system to treat ocular infections. PLoS One 2021;16:e0248857.

Son GH, Lee BJ, Cho CW. Mechanisms of drug release from advanced drug formulations such as polymeric-based drug-delivery systems and lipid nanoparticles. Int J Pharm Investig 2017;47:287–96.

Li SS, Li GF, Liu L, Jiang X, Zhang B, Liu ZG, et al. Evaluation of paeonol skin-target delivery from its microsponge formulation: in vitro skin permeation and in vivo microdialysis. PLoS One 2013;20;8:e79881.

Song J, Bi H, Xie X, Guo J, Wang X, Liu D. Preparation and evaluation of sinomenine hydrochloride in situ gel for uveitis treatment Int. Immunopharmacol 2013;17:99–107.

Indian Pharmacopoeia. The controller of publication, New Delhi; Ministry of health and family welfare. India. 6th Eed. Volume II; 2010. p. 59-66.

Kucukturkmen B, Oz UC, Bozkir A. In situ hydrogel formulation for intra-articular application of diclofenac sodium-loaded polymeric nanoparticles. Turk J Pharm Sci 2017;14:56-64.

Kumar PM, Ghosh A. Development and evaluation of metronidazole loaded microsponge based gel for superficial surgical wound infections. J Drug Delivery Sci Technol 2015;30:15-29.

Deshmukh K, Poddar SS. Tyrosinase inhibitor-loaded microsponge drug delivery system: new approach for hyperpigmentation disorders. J Microencapsul 2012; 29:559–68.

Charoo NA, Kohli K, Ali A. Preparation of in situ-forming ophthalmic gels of ciprofloxacin hydrochloride for the treatment of bacterial conjunctivitis: in vitro and in vivo studies. J Pharm Sci 2003;92:407–13.

Makwana SB, Patel VA, Parmar SJ. Development and characterization of in-situ gel for ophthalmic formulation containing ciprofloxacin hydrochloride Results Pharma Sci 2016;6:1–6.

Sheshala R, Ming NJ, Kok YY, Singh TRR, Dua K. Formulation and characterization of pH induced in situ gels containing sulfacetamide sodium for ocular drug delivery: a combination of carbopol®/HPMC polymer. Indian J Pharm Educ Res 2019;53:654-62.



How to Cite

AMBIKAR, R. B., and A. V. BHOSALE. “DEVELOPMENT AND CHARACTERIZATION OF DICLOFENAC SODIUM LOADED EUDRAGIT RS100 POLYMERIC MICROSPONGE INCORPORATED INTO IN SITU GEL FOR OPHTHALMIC DRUG DELIVERY SYSTEM”. International Journal of Pharmacy and Pharmaceutical Sciences, vol. 13, no. 9, Sept. 2021, pp. 63-69, doi:10.22159/ijpps.2021v13i9.42405.



Original Article(s)