Skip to main content
SpringerLink
Log in

Formulation and evaluation of sparfloxacin emulsomes-loaded thermosensitive in situ gel for ophthalmic delivery

  • Original Paper
  • Published:
Journal of Sol-Gel Science and Technology Aims and scope Submit manuscript

Abstract

The aim of the present study was to develop thermosensitive emulsomal in situ gel for ocular delivery of sparfloxacin, an antibacterial drug. The study was conducted in two steps. In the first step, sparfloxacin emulsomes were prepared by thin film hydration technique and characterized. Compritol 888 ATO (CA) was used as lipid core and Phospholipon 90G (PC) as stabilizer. The optimized emulsomal formulation (E3) showed mean particle size of 217 ± 3.78 nm, with 72.83 ± 2.56 % drug entrapment efficiency, and showed a slow and consistent release of the drug over period of 24 h in simulated tear fluid (STF) pH 7.4. In the second step, the drug-loaded emulsomal suspension was dispersed in Pluronic (PF 127 and PF 68) solution yielding the emulsomal in situ gel. The optimized gel formulation GF1 gelled at around 35 °C. Drug content was found to be 92.42 ± 2.08 %. The viscosity of the formulation at 25 ± 1 and 37 ± 1 °C was 107.46 ± 6.74 and 1669 ± 13.89 cps, respectively. The in vitro drug release revealed a sustained profile over a period of 12 h. The formulation was non-irritant and showed promising in vitro and in vivo antimicrobial activity. Stability studies indicated that 4 ± 1 °C is appropriate storage condition for the formulation. The findings suggested that the novel emulsomal in situ gelling system could be a viable alternative to conventional eye drops.

Graphical Abstract

This is a preview of subscription content, log in via an institution to check access.

Access this article

Log in via an institution

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Institutional subscriptions

Fig. 1
Fig. 2
Fig. 3
Fig. 4
Fig. 5
Fig. 6
Fig. 7
Fig. 8
Fig. 9

Similar content being viewed by others

Abbreviations

CA:

Compritol 888 ATO

PC:

Phospholipon 90G

PF68:

Pluronic F 68

PF127:

Pluronic F127

STF:

Simulated tear fluid

PBS:

Phosphate-buffered saline

BCS:

Biopharmaceutical classification scheme

TEM:

Transmission electron microscope

References

  1. Kaur IP, Garg A, Singla AK, Aggarwal D (2004) Vesicular systems in ocular drug delivery: an overview. Int J Pharm 269(1):1–14

    Article  Google Scholar 

  2. Almeida H, Amaral MH, Lobão P, Lobo JMS (2013) In situ gelling systems: a strategy to improve the bioavailability of ophthalmic pharmaceutical formulations. Drug Discov Today 19(4):400–412

    Article  Google Scholar 

  3. Urtti A (2006) Challenges and obstacles of ocular pharmacokinetics and drug delivery. Adv Drug Deliv Rev 58(11):1131–1135

    Article  Google Scholar 

  4. Gill B, Singh J, Sharma V, Hari Kumar SL (2012) Emulsomes: an emerging vesicular drug delivery system. Asian J Pharm 6:87–94

    Article  Google Scholar 

  5. Nair AS, Vidhya KM, Saranya TR, Sreelakshmy KR, Sreeja CN (2013) Emulsomes: a novel liposomal formulation for sustained drug delivery. Int Res J Pharm App Sci 3(5):192–196

    Google Scholar 

  6. Nagarwal RC, Kumar R, Dhanawat M, Pandit JK (2011) Modified PLA nano in situ gel: a potential ophthalmic drug delivery system. Colloids Surf B 86:28–34

    Article  Google Scholar 

  7. Patil AP, Tagalpallewar AA, Rasve GM, Bendre AV, Khapekar PG (2012) A novel ophthalmic drug delivery system: in situ gel. Int J Pharm Sci Res 3(09):2938–2946

    Google Scholar 

  8. Zhanel GG et al (1999) The new fluoroquinolones: a critical review. Can J Infect Dis 10(3):207–238

    Google Scholar 

  9. Sweetman SC (2009) Martindale: the complete drug reference. Everbest, China

    Google Scholar 

  10. Paliwal R, Paliwal SR, Mishra N, Mehta A, Vyas SP (2009) Engineered chylomicron mimicking carrier emulsome for lymph targeted oral delivery of methotrexate. Int J Pharm 380(1–2):181–188

    Article  Google Scholar 

  11. Raza K, Katare OP, Setia A, Bhatia A, Singh B (2013) Improved therapeutic performance of dithranol against psoriasis employing systematically optimized nanoemulsomes. J Microencapsul 30(3):225–236

    Article  Google Scholar 

  12. Varshosaz J, Tabbakhian M, Salmani Z (2008) Designing of a thermosensitive chitosan/poloxamer in situ gel for ocular delivery of ciprofloxacin. Open Drug Deliv J 2:61–70

    Article  Google Scholar 

  13. Saxena P, Kushwaha SK (2013) Temperature sensitive ophthalmic hydrogels of levofloxacin hemihydrate with enhanced solubility and prolonged retention time. Int J Pharm Pharm Sci 5:1–7

    Google Scholar 

  14. Nayak SN, Sogali BS, Thakur RS (2012) Formulation and evaluation of pH triggered in situ ophthalmic gel of moxifloxacin hydrochloride. Int J Pharm Pharm Sci 4(2):452–459

    Google Scholar 

  15. Rathore KS (2011) Development and in vivo in vitro characterizations of timolol maleate in situ gels. Int J Pharm Bio Sci 2(3):248–263

    Google Scholar 

  16. Vodithala S, Khatry S, Shastri N, Sadanandam M (2010) Development and evaluation of thermoreversible ocular gels of ketorolac tromethamine. Int J Biopharm 1(1):39–45

    Google Scholar 

  17. Gupta H, Aqil M, Khar RK, Ali A, Bhatnagar A, Mittal G (2010) Sparfloxacin-loaded PLGA nanoparticles for sustained ocular drug delivery. Nanomedicine Nanotechnol Biol Med 6(2):324–333

    Article  Google Scholar 

  18. Parthiban KG, Manivannan R, Kumar BS, Ahasan MA (2010) Formulation and evaluation of ketorolac ocular pH-triggered in situ gel. Int J Drug Dev Res 2(3):459–467

    Google Scholar 

  19. Charoo NA, Kohli K, Ali A (2003) 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 92:407–413

    Article  Google Scholar 

  20. Kulkarni GT, Suresh B (2004) Stability testing of pharmaceutical products: an overview. Indian J Pharma Educ 38(4):194–202

    Google Scholar 

  21. Pawar P, Kashyap H, Malhotra S, Sindhu R (2013) Formulation design of thermo sensitive voriconazole in situ gelling system for ocular drug delivery: in vitro, stability and antifungal activities assessment. BioMed Res Int 2013:1–8

    Article  Google Scholar 

  22. Venkatesh MP, Purohit KL, Kumar P (2013) Development and evaluation of chitosan based thermosensitive in situ gels of pilocarpine. Int J Pharm Pharm Sci 1(5):164–169

    Google Scholar 

Download references

Acknowledgments

Authors are thankful to the KLE University, Belagavi; Indian Council of Medical Research, Belagavi; and Dr. Prabhakar Kore Basic Science Research Centre, Belagavi, for providing research facilities to carry out this research work. Authors extend acknowledgment to FDC Pvt Ltd, Goa; Gattefosse, India, and Lipoid, Germany, for providing Sparfloxacin, Compritol and Phospholipon 90G as gift samples, respectively.

Author information

Authors and Affiliations

  1. Department of Pharmaceutics, KLES College of Pharmacy, Nehrunagar, Belagavi, Karnataka, India

    Dipiksha Sawant, Panchaxari Mallappa Dandagi & Anand Panchaxari Gadad

Authors
  1. Dipiksha Sawant
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. Panchaxari Mallappa Dandagi
    View author publications

    You can also search for this author in PubMed Google Scholar

  3. Anand Panchaxari Gadad
    View author publications

    You can also search for this author in PubMed Google Scholar

Corresponding author

Correspondence to Dipiksha Sawant.

Rights and permissions

Reprints and permissions

About this article

Check for updates. Verify currency and authenticity via CrossMark

Cite this article

Sawant, D., Dandagi, P.M. & Gadad, A.P. Formulation and evaluation of sparfloxacin emulsomes-loaded thermosensitive in situ gel for ophthalmic delivery. J Sol-Gel Sci Technol 77, 654–665 (2016). https://doi.org/10.1007/s10971-015-3897-8

Download citation

  • Received:

  • Accepted:

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.1007/s10971-015-3897-8

Keywords

Search

Navigation