Generic placeholder image

Nanoscience & Nanotechnology-Asia

Editor-in-Chief

ISSN (Print): 2210-6812
ISSN (Online): 2210-6820

Research Article

Preparation and Evaluation of Gliptin Liposomes for Targetting Ocular Region in Neurodegeneration

Author(s): Deepika Sharma, Swarna Raj, Manmohan Singhal and Bhavna Kumar*

Volume 11, Issue 2, 2021

Published on: 14 April, 2020

Page: [197 - 203] Pages: 7

DOI: 10.2174/2210681210999200414104232

Price: $65

Abstract

Background: Neurodegeneration shows the distressing effects of miscommunications between brain cells. Insulin signaling dysregulation and small vessel disease in the base of diabetes may be important contributing factors in Alzheimer’s disease and vascular dementia. Gliptins play a role in neurodegeneration due to its neuroprotective effects. Eye is an extension of the brain. Ocular route reduces drug’s adverse effects offering an advantage in minimizing risk by targeted delivery to the brain. Conventional ophthalmic formulations exhibit poor bioavailability. Liposomes serve as promising active carriers of drugs to posterior segment eye disorders due to improvement in intravitreal half-life and targeted sustained drug delivery to the retina. Liposomes act as drug carriers for entrapment of hydrophilic and hydrophobic drugs.

Objective: The study aimed to formulate and evaluate sitagliptin liposomal formulation for sustained effect in individuals suffering from neurodegeneration owing to high patient compliance, especially in geriatric patients.

Methods: Sitagliptin liposomes were prepared by the ethanol injection method and were evaluated for various physicochemical properties such as visual appearance, particle size distribution, zeta potential, % drug entrapment efficiency, % drug loading capacity and in vitro drug release studies.

Results: The optimized formulation (L-3) showed round-shaped distinct particles with good stability. The L-3 shows average diameter (281.9 nm); zeta potential (-11.9 mV); % entrapment efficiency (82.7 ± 0.89%); % drug loading (33.11 ± 0.67%). L-3 followed Korsmeyer- Peppas model with fickian diffusion transport of drug release giving n’ (0.3094), r2 (0.9753), with 83.78 ± 0.97% of sustained drug release. The L-3 passes the sterility test indicating its safe use in ophthalmic purposes.

Conclusion: Thus, liposomal drug delivery is a highly effective approach for sustained drug delivery and minimizing the side effects of gliptins for effective therapy in neurodegeneration.

Keywords: Sitagliptin, liposomes, ocular, neurodegeneration, DPP-4, in vitro drug release, in vitro drug release model.

Graphical Abstract
[1]
Kumar, B.; Sharma, D. Recent advances in neurodegenerative disorders and its treatment. Recent Pat. Drug Deliv. Formul., 2017, 11(3), 158-172.
[http://dx.doi.org/10.2174/1872211311666171010123958]. [PMID: 29032765]
[2]
Sharma, D. Bhavna. Formulation and evaluation of gliptin loaded polymeric nanomicelles for controlled drug delivery. Drug Deliv. Lett., 2019, 9, 1-11.
[http://dx.doi.org/10.2174/2210303109666190212112505]
[3]
Mousa, S.A.; Ayoub, B.M. Repositioning of dipeptidyl peptidase-4 inhibitors and glucagon like peptide-1 agonists as potential neuroprotective agents. Neural Regen. Res., 2019, 14(5), 745-748.
[http://dx.doi.org/10.4103/1673-5374.249217]. [PMID: 30688255]
[4]
Kumar, A.; Badde, S.; Kamble, R.; Pokharkar, B.V. Development and characterization of liposomal drug delivery system for nimesulide. Int. J. Pharm. Pharm. Sci., 2010, 2, 8789.
[5]
Ben, S. Treatments for Retinal Diseases are leading to Therapies for the Brain; Foundation Fighting Blindness, 2016.
[6]
Gyan, P. Mishra, Mahuya Bagui, Viral Tamboli, Ashim KM. Recent applications of liposomes in ophthalmic drug delivery. J. Drug Deliv., 2016, 2016, 1-14.
[7]
Kaur, I.P.; Kanwar, M. Ocular preparations: The formulation approach. Drug Dev. Ind. Pharm., 2002, 28(5), 473-493.
[http://dx.doi.org/10.1081/DDC-120003445]. [PMID: 12098838]
[8]
Wadhwa, S.; Paliwal, R.; Paliwal, S.R.; Vyas, S.P. Nanocarriers in ocular drug delivery: An update review. Curr. Pharm. Des., 2009, 15(23), 2724-2750.
[http://dx.doi.org/10.2174/138161209788923886]. [PMID: 19689343]
[9]
Laouini, A.; Jaafar, C.; Limayem, I.; Sfar, S.; Charcosset, C. Preparation, characterization and applications of liposomes: State of the Art. J. Colloid Sci. Biotechnol., 2012, 1, 147-168.
[http://dx.doi.org/10.1166/jcsb.2012.1020]
[10]
Lian, T.; Ho, R.J. Trends and developments in liposome drug delivery systems. J. Pharm. Sci., 2001, 90(6), 667-680.
[http://dx.doi.org/10.1002/jps.1023]. [PMID: 11357170]
[11]
Karimi, N.; Ghanbarzadeh, B.; Hamishehkar, H. Phytosome and Liposome: The beneficial encapsulation systems in drug delivery and food application. Appl. Food Biotechnol., 2015, 2, 17-27.
[12]
Li, J.; Wang, X.; Zhang, T.; Huang, Z. A review on phospholipids and their main applications in drug delivery systems. Asian J. Pharmaceut. Sci., 2015, 10, 81-98.
[http://dx.doi.org/10.1016/j.ajps.2014.09.004]
[13]
Akbarzadeh, A.; Rezaei-Sadabady, R.; Davaran, S.; Joo, S.W.; Zarghami, N.; Hanifehpour, Y.; Samiei, M.; Kouhi, M.; Nejati-Koshki, K. Liposome: Classification, preparation, and applications. Nanoscale Res. Lett., 2013, 8(1), 102.
[http://dx.doi.org/10.1186/1556-276X-8-102]. [PMID: 23432972]
[14]
Bulbake, U.; Doppalapudi, S.; Kommineni, N.; Khan, W. Liposomal formulations in clinical use: An updated review. Pharmaceutics, 2017, 9(2), 1-33.
[http://dx.doi.org/10.3390/pharmaceutics9020012]. [PMID: 28346375]
[15]
Anwekar, H.; Patel, S.; Singhai, A.K. Liposome- as drug carriers. Int. J. Pharm. Life Sci., 2011, 2, 945-951.
[16]
Popovska, O.; Simonovska, J.; Kavrakovski, Z.; Rafajlovska, V. An overview: Methods for preparation and characterization of liposomes as drug delivery systems. Int. J. Pharmaceut. Phytopharmacol. Res., 2013, 3, 182-189.
[17]
Lamoudi, L.; Chaumeil, C.J.; Daoud, K. PLGA Nanoparticles loaded with the non-steroid anti-inflammatory: Factor influence study and optimization using factorial design. Int. J. Chem. Eng. Appl., 2013, 4, 369-372.
[http://dx.doi.org/10.7763/IJCEA.2013.V4.327]
[18]
Panwar, P.; Pandey, B.; Lakhera, P.C.; Singh, K.P. Preparation, characterization, and in vitro release study of albendazole-encapsulated nanosize liposomes. Int. J. Nanomed., 2010, 5, 101-108.
[PMID: 20309396]
[19]
Reddy, A.S.; Sailaja, A.K. Preparation and characterisation of aspirin loaded ethylcellulose nanoparticles by solvent evaporation technique. World J. Pharm. Pharm. Sci., 2014, 3, 1781-1793.
[20]
Shanmugam, S.; Valarmathi, S.; Kumars, S. Sterility testing procedure of ophthalmic ocusert aciclovir used for treating herpes simplex virus. Asian J. Pharm. Clin. Res. (Alex.), 2017, 10, 344-346.
[21]
Chrai, S.S.; Makoid, M.C.; Eriksen, S.P.; Robinson, J.R. Drop size and initial dosing frequency problems of topically applied ophthalmic drugs. J. Pharm. Sci., 1974, 63(3), 333-338.
[http://dx.doi.org/10.1002/jps.2600630304]. [PMID: 4820359]
[22]
Dandagi, P.M. Development and evaluation of ocular films of cromolyn sodium. Indian J. Pharm. Sci., 2004, 66, 309-312.
[23]
Nithiyananthan, T.S.; Shankarananth, V.; Rajasekhar, K.K.; Jyothikrishna, K.; Mukesh, O.; Kumar, E.V. Preparation and evaluation of ciprofloxacin ousters. J. Pharm. Res., 2009, 2, 1496-1499.
[24]
Chandran, C.S.; Shirwalkar, A.; Kiron, S.S. Development and evaluation of chitosan containing ciprofloxacin-B CD complex. Int. J. Pharm. Tech. Res., 2010, 2, 246-252.
[25]
Hathout, R.M.; Mansour, S.; Mortada, N.D.; Guinedi, A.S. Liposomes as an ocular delivery system for acetazolamide: In vitro and in vivo studies. AAPS PharmSciTech, 2007, 8(1), 1.
[http://dx.doi.org/10.1208/pt0801001]. [PMID: 17408209]
[26]
Johnston, M.J.; Semple, S.C.; Klimuk, S.K.; Ansell, S.; Maurer, N.; Cullis, P.R. Characterization of the drug retention and pharmacokinetic properties of liposomal nanoparticles containing dihydrosphingomyelin. Biochim. Biophys. Acta, 2007, 1768(5), 1121-1127.
[http://dx.doi.org/10.1016/j.bbamem.2007.01.019]. [PMID: 17321495]
[27]
Kim, C.K.; Park, D.K. Stability and drug release properties of liposomes containing cytarabine as a drug carrier. Arch. Pharm. Res., 1987, 10, 75-79.
[http://dx.doi.org/10.1007/BF02857770]
[28]
Honary, S.; Zahir, F. Effect of zeta potential on the properties of nano-drug delivery systems - A review. Trop. J. Pharm. Res., 2013, 12, 265-273.
[29]
Dash, S.; Murthy, P.N.; Nath, L.; Chowdhury, P. Kinetic modeling on drug release from controlled drug delivery systems. Acta Pol. Pharm., 2010, 67(3), 217-223.
[PMID: 20524422]
[30]
Gao, Y.; Zuo, J.; Chacra, N.; Pinto, T.; Clas, S.; Walker, R.; Löbenberg, R. In vitro release kinetics of antituberculosis drugs from nanoparticles assessed using a modified dissolution apparatus. BioMed Res. Int., 2013, 2013, 1-9.
[31]
Sharma, D.; Bhargava, S. Bhavna. Development and optimization of nanomicelles of dpp-4 inhibitor using response surface methodology. Drug Dev. Ind. Pharm., 2019, 46(1), 70-79.
[http://dx.doi.org/10.1080/03639045.2019.1701003]. [PMID: 31795778]
[32]
Shanmugam, S.; Valarmathi, S.; Kumars, S. Sterility testing procedure of ophthalmic ocusert aciclovir used for treating herpes simplex virus. Asian J. Pharm. Clin. Res., 2017, 10(10), 344-346.

Rights & Permissions Print Cite
© 2024 Bentham Science Publishers | Privacy Policy