Design, Development and Characterization of Hyaluronic Acid Based pH Sensitive Liposomal In Situ Gel for the Treatment of Keratoconjunctivitis Sicca
Abstract
The recent advances in ocular drug delivery have been successful in surpassing conventional therapy, owing to its considerable limitations. This study aims to develop and optimize in-situ liposomal ocular system to design once-daily liquid preparation to treat Keratoconjunctivitis sicca. Liposomes of Hyaluronic acid were prepared using soya lecithin by a thin film hydration method. Eight trial formulations were made by keeping drug as fixed ratio and varying the concentration of cholesterol and soya lecithin. The optimized formulation was selected for the formulation of liposomal in-situ hydrogel. Optimization was carried out by Central Composite Design (CCD) studying the factors, amount of cholesterol and soya lecithin and its effects on the responses, % In- vitro drug release (R1) and Percent Entrapment Efficiency (% EE) (R2). The best predicted model for R1 was the Quadratic model and, for R2 was Two-Factor Interaction model (2FI) without any significant lack of fit. Optimum formulation was found to be at 1:1:4 (drug: cholesterol: soya lecithin) showed sustained drug release of 31.28% in 8 hours with highest %EE of 47.36%. Liposomal in-situ gel preparation retained better stability throughout the study period when stored at refrigerator temperature and displayed prolonged action (76.44%) when compared to liposomal formulation (68.72%).
Keywords: Liposomes, Hyaluronic acid, Optimized formulation, CCD, sustained drug release, in-situ hydrogel.
Keywords:
Liposomes, Hyaluronic acid, Optimized formulation, CCD, sustained drug release, in-situ hydrogelDOI
https://doi.org/10.22270/jddt.v13i1.5888References
Professor Saettone. Progress and problems in ophthalmic drug delivery. Business Briefing. Pharma tech. 2002; 1-6.
Samar M, Guinedi AS, Preparation and evaluation of reverse phase evaporation and
multilamellar Niosomes as ophthalmic carriers of acetazolamide, Int J Pharma,2005; 306:71. https://doi.org/10.1016/j.ijpharm.2005.09.023
Widjaja LK et.al., Hyaluronic acid-based nanocomposite hydrogels for ocular drug delivery applications, J Biomed Mater Res A, 2014; 102(9):3056-65. https://doi.org/10.1002/jbm.a.34976
Sharma A, Sharma US, Liposomes in drug delivery: progress and limitations, International journal of pharmaceutics, 1997; 154(2):123-40. https://doi.org/10.1016/S0378-5173(97)00135-X
Pal Kaur I, Kanwar M,Ocular preparations: the formulation approach, Drug development and industrial pharmacy, 2002; 28(5):473-93. https://doi.org/10.1081/DDC-120003445
Khan N, Aqil M ,Imam SS ,Ali A, Development and evaluation of a novel in situ gel of sparfloxacin for sustained ocular drug delivery: in vitro and ex vivo characterization, Pharm Dev Technol , 2015; 20(6):662-9 . https://doi.org/10.3109/10837450.2014.910807
Gayton JL, Etiology, prevalence, and treatment of dry eye disease, Clinical ophthalmology (Auckland, NZ), 2009; 3:405 https://doi.org/10.2147/OPTH.S5555
Rathore KS, Nema RK, An insight in to ophthalmic drug delivery system, IJPSDR, 2009; 1(1):1-5. https://doi.org/10.25004/IJPSDR.2009.010101
Hong RL, Sung KC, Carbopol/ pluronic phase change solutions for ophthalmic drug delivery, J. Control. Release, 2000; (69):379-388 https://doi.org/10.1016/S0168-3659(00)00329-1
Gayton JL, Etiology, prevalence, and treatment of dry eye disease, Clinical ophthalmology (Auckland, NZ). 2009; 3:405 https://doi.org/10.2147/OPTH.S5555
Rathore KS, In-situ gelling ophthalmic drug delivery system: An overview, Int J Pharm Sci., 2010; 2(4):30-34.
Almira I, Blazek W, David GR, SEM Imaging predicts Quality of niosomes from maltodextrin - based proniosmes, Pharm. Res., 2001; 18(5):656-661. https://doi.org/10.1023/A:1011037527889
Yasin MN, Hussain S, Malik F, Hameed A, Sultan T, Qureshi F, Preparation and characterization of chloramphenicol niosomes of comparison with eye drops, Pak J. Pharm Sci., 2012; 25(1):117-121.
Alsarra IA, Bosela AA, Ahmed SM, Mahrous GM, Proniosomes as a drug carrier for transdermal delivery of kertolac, Eur J Pharm Biopharm, 2005; 59(3):485-490. https://doi.org/10.1016/j.ejpb.2004.09.006
Jaleh Varshosaz et. al., Development and optimization of solid lipid nanoparticles of amikacin by central composite design, Journal of Liposome Research, 2010; 20(2):97-104 https://doi.org/10.3109/08982100903103904
Law SL, Shin CL, Characterization of Calcitonin containing liposome formulation for intranasal delivery. J. Microencapsul, 2001; 18(2):211-221. https://doi.org/10.1080/02652040010000334
Yoshida CM, Kok W, Junginger HE, Verhoef JC, Bouwistra JA., Niosomes for oral delivery of peptide drugs, J.Control Rel, 1992; 21:145-153. https://doi.org/10.1016/0168-3659(92)90016-K
Cascino GD, Epilespy contemporary perspectives on evaluation and treatment, Mayo clinic Proc 1994; 69:1199-1211. https://doi.org/10.1016/S0025-6196(12)65776-0
Satia MC, Vandana D, Mody Rajiv I, Kabra PK, Khamer M, Pharmacokinetics of topically applied sparfloxacin in rabbits, Int Journal of Pharmacology online IP; 117, 213.95.28.
Maryam K, Reza B, Neda B, Ferjdorn F, Ocular Dorzolamide nanoliposomes for prolonged IOP reduction: In vitro and In vivo evaluation in rabbits, Iran J Pharm Res, 2016; 15(1):205-212.
Guinedi AS, Mortada ND, Mansour S, Hathout RM. Sameo M, Ahmed GS, Preparation and evaluation of reverse phase evaporation and multimedia niosomes as ophthalmic carrier of acetazolamide, Int. J. Pharm, 2005; 306(1- 2):78-82. https://doi.org/10.1016/j.ijpharm.2005.09.023
Gupta N, Shrivastava V, Sarena S, Formulation and evaluation of non-ionic surfactant vesicles for ocular delivery of ofloxacin, Int. J. Pharm life Sci., 2010; 1(7):143-418.
Verma P, Gupta RN, Jha AK, Development of In-vitro and biological evaluation of chitosan reinforced Eudragit RL 100 nanoparticles for the improvement of ocular bioavailability of acetozoloamide, British Biomedical Bulletin, 2014 ; (2):329-342
Vyshnavi V, Indira S, Prathima S, Formulation and evaluation of nasal niosomal in-situ gel of Loratadine, Int Journal of Pharmaceutical Sciences and drug research, 2015; 7(1):13-18.
Lavanya B, Indira, Prathima S, Formulation and evaluation of ocular niosomal in-situ gel of linezolid, IJPSR, 2014; 5(4):1367-1375.
Published
Abstract Display: 575 
PDF Downloads: 672 PDF Downloads: 250 How to Cite
Issue
Section
Authors who publish with this journal agree to the following terms:
- Authors retain copyright and grant the journal right of first publication with the work simultaneously licensed under a Creative Commons Attribution-NonCommercial 4.0 International (CC BY-NC 4.0). that allows others to share the work with an acknowledgment of the work's authorship and initial publication in this journal.
- Authors are able to enter into separate, additional contractual arrangements for the non-exclusive distribution of the journal's published version of the work (e.g., post it to an institutional repository or publish it in a book), with an acknowledgment of its initial publication in this journal.
- Authors are permitted and encouraged to post their work online (e.g., in institutional repositories or on their website) prior to and during the submission process, as it can lead to productive exchanges, as well as earlier and greater citation of published work (See The Effect of Open Access).
How to Cite
.