Novel Strategy In Controlled Gastroretentive Drug Delivery: In-Situ Floating Gel
Keywords:
Hollow microspheres, Multiparticulate floating system, peroral delivery, Gastro retentive floating DDSAbstract
Attempts are made in research and development of sustained and controlled drug delivery systems to overcome physiological and unpredictable gastric empting time (GET). Such dosage forms are useful for the drugs with Ânarrow therapeutic index'. Formation of gel depends on factors such as temperature, pH, ionic cross linking and UV irradiation, from which drug is released in controlled or sustained manner. In-situ gelling systems is prominent among other novel drug delivery systems (NDDS), due to advantages such as sustained and prolonged drug action, improved patient compliance and reduced frequency of drug administration as compared to conventional drug delivery system. These polymeric formulations are in solution form before administration and then turns to gel form when comes in contact with gastric fluids. Various natural, biodegradable, biocompatible and water soluble polymers such as pectin, gallen gum, chitosan, poly-caprolactone, xyloglucane, poly-D, L-lactic acid, pluronic F 127, carbopol, etc makes this drug delivery most acceptable and useful. In-situ gel is fabricated for both local and systemic drug delivery at specific site of action. Various evaluations are recommended for in-situ gels mostly viscosity, buoyancy, gelling capacity and dissolution studies are performed. This review presents current trends in fabrication, evaluation parameters and importance of various drugs formulated as in-situ gelling system.
References
Gopalakrishnan,S.; Chenthilnathan, A. Floating Drug Delivery Systems: A Review. J Pharm Sci Tech. 2011, 3 (2), 548- 554.
Chandel Abhishek, Chauhan Kapil, Parashar Bharat, Hiteshkumar, Arora Sonia, Floating drug delivery systems: A better approach. Int Current Pharm J, 2012; 1(5):110-118.
Parmar PD, Pande S, Shah SH, Sonara N, Floating drug delivery system: A novel approach to prolong gastric retention. World J Pharmacy Pharm Sci. 2014; 3(4):418-444.
Singh BM, Kim KH. Floating drug delivery systems: An approach to oral controlled drug delivery via gastric retention. J Cont Rel. 2000; 63: 235-259.
Ramya DD, In-situ gelling system- Potntial tool for improving therapeutic effects of drugs. Int J Pharmacy Pharm Sci. 2013; 5(3): 27-30.
Bharadwaj L, Sharma PK, A short review on gastro retentive formulations for stomach specific drug delivery: Special emphasis on floating in-situ gel system. Afr J Bas Appl Sci. 2011; 3(6):300-312.
Vyas, S.P.; Khar, R.Ks. Gastroretentive systems. In: Controlled drug Delivery. Vallabh Prakashan, Delhi, India. 2006. p 197-217.
Wand D et al, Parenteral thermo-sensitive organogel for schizophrenia therapy, in vitro and in-vitro evalvation. Eup J Pharm Sci. 2014;
http://dx.doi.org/10.1016/j.ejps/2014.04.020
Anda V, Michel L, Guillaume B, Jean-Christophe L. In-situ-forming oleogel implant for Rivastigmine delivery. Pharm Res 2008; 25(4) :845-852.
Miyazaki S, Suzuki S, Kawasaki N, Endo K, Takahashi A, Attwood D. In-situ gelling xyloglucan formulations for sustained release ocular delivery of Pilocarpine hydrochloride. Int J Pharm 2001; 229(1-2): 29-36.
Malik APH, Satyanand S. pH induced in-situ gelling system of an anti-infective drug for sustain ocular delivery. J Appl Pharm Sci. 2014; 4(1): 101-104.
Shashank Nayak N, Bharani S Sogali, R S Thakur, Formulation And Evaluation Of pH Triggered In Situ Ophthalmic Gel Of Moxifloxacin Hydrochloride. Int J Pharm Pharm Sci. 2012; 4(2): 452-459.
Rathore KS, Insitu gelling ophthalmic drug delivery system: An overview Int J Pharm Pharm Sci, 2010; 2: 30-34.
Lin T, Effectiveness and safety of 0.15% ganciclovir in-situ ophthalmic gel for herpes simplex karetitis- a multicenter randomized, investigator masked, parallel group study in Chinese patients. Drug Design, Development and Study.2013;7: 361-368.
Eaga CM, Jagan MK, Venkatesham A. Preparation and evaluation of in-situ gels for ocular drug delivery. J Pharm Res 2009; 2: 1089-1094.
Shivanand SP, Fatima SD, Abidabegum N, Vilas GJ, Jameel SM, Sreenivas SA, et al. Formulation and evaluation of a novel in-situ gum based ophthalmic drug delivery system of Linezolid. Scientia Pharmaceutia 2008; 76: 515–532.
Rahul N, Venkatakrishnakiran P, Dhanalakshmi P, Prasannaraju Y. Formulation and evaluation of in-situ gelling systems for ocular delivery of Doxycycline hyclate. J Inno Trends Pharm Sci 2012; 3: 1-7.
Sonjoy KMJ, Thimmasetty GL, Prabhu S, Geetha MS. Formulation and evaluation of an in-situ gel forming ophthalmic formulation of Moxiflaxin hydrochloride. Int J Pharma Investig 2012; 2: 2.
Wagh VD, Deshmukh KH, Wagh KV. Formulation and evaluation of in-situ gel drug delivery system of Sesbania grandiflora flower extract for the treatment of bacterial conjunctivitis. J Pharm Res 2012; 4: 1880-1884.
Ramesh CN, Rakesh K, Dhanawat M, Pandit JK. Modified PLA nano in-situ gel: A potential ophthalmic drug delivery system. Colloids and Surfaces B: Bointerfaces. 2011; 86: 28–34.
Bain MK, Bhowmik M, Ghosh SN, Chattopadhyay D. In-situ fast gelling formulation of methyl cellulose for in-vitro ophthalmic controlled delivery of Ketorolac Tromethamine. J Appl Polym Sci. 2009; 113(2): 1241-1246.
Nagesh C, Patil M, Chandrashekhara S, Sutar R. A novel in-situ gel for sustained ophthalmic delivery of Ciprofloxacin hydrochloride and Dexamethasone- design and characterization. Der Pharmacia Lettre. 2012; 4(3): 821-827.
Jun F, Xuemei F, Haihong Y, Liming Y, Xiaodong K, Zheng X, et al. Study of ocular pharmacokinetics of in-situ gel system for S(−)-satropane evaluated by microdialysis. J Pharm Biomed Anal. 2008; 48(3): 840-843.
Seham S, Abd E, Nahed DM, Gehanne ASA, Noha MZ, Ragia AT. Development of in-situ gelling and mucoadhesive Mebeverine hydrochloride solution for rectal administration. Saudi Pharma J. 2003; 11: 159-171.
Lin HR, Tseng CC, Lin YJ, Ling MH. A novel in-situ gelling liquid suppository for site-targeting delivery of anti-colorectal cancer drugs. J Biomater Sci Polym Ed 2012; 23: 807-822.
Choi HG, Oh YK, Kim CK. In-situ gelling and mucoadhesive liquid suppository containing Acetaminophen: Enhanced bioavailability. Int J Pharm 1998; 165: 23-32.
Yuan Y, Cui Y, Zhang L, Zhu HP, Guo YS, Zhong B, et al. Thermosensitive and mucoadhesive in-situ gel based on poloxamer as new carrier for rectal administration of Nimesulide. Int J Pharm 2012; 430(1-2): 114-119.
Sinem YK, Seda R, Zeynep AS, Esra B. A new in-situ gel formulation of Itraconazole for vaginal administration. J Pharm Pharmacol 2012; 3: 417-426
El-sayed AI, Sayed I, Gihan F, Omar S, Khaled H, Noura HA. Development and characterization of thermosensitive pluronic-based Metronidazole in-situ gelling formulations for vaginal application. Acta Pharm 2012; 62: 59–70.
Moink M, Bhupendrag P, Vishnum P, Jayvadan KP. Floating in-situ gel based on alginate as carrier for stomach specific drug delivery of famotidine. Int J Pharm Sci Nanotech. 2010; 3(3): 1092-1104.
Miyazaki S, Kawasaki N, Kubo W, Endo K, Attwood D. Comparison of in-situ gelling formulations for the oral delivery of Cimetidine. Int J Pharm 2011; 220: 161-168.
Prathiba P, Deepak C, Gaurav J, Shoerey RV. Formulation and evaluation of oral in-situ gel of Diltiazem HCl. Int J Nov Drug Del 2011; 2(1):264-270
Vinay W, Mohan VM, Manjunath SY. Formulation and evaluation of stomach specific in-situ gel of Metoclopramide using natural bio-degradable polymers. Int J Res Pharm Biome Sci. 2011; 2(2):193-201.
El Maghraby GM, Elzayat EM, Alanazi FK. Development of modified in-situ gelling oral liquid sustained release formulation of Dextromethorphan. Drug Dev Ind Pharm. 2012; 38: 971-978.
Haoping Xu , A novel in-situ gel for formulation of ranitidine for oral sustained delivery. Biomol ther (Seoul), 2014, 22(2); 161-5.
Rao PB, Bindu HE. Design optimization and evaluation of mucoadhesive peroral in-situ gel containing anti fungal drug for candidiasis. Indo Ameri J Pharm Res. 2014; 4(1):884-895.
Harish NM, Prabhu P, Charluyu RN, Subramanyam EVS. Formulation and evaluation of in-situ gel containing Clotrimazole for oral candidiasis, J Pharm Sci 2012; 4: 1885-1889.
Pillai O, Panchagnula R, Transdermal delivery of insulin from poloxamer gel: ex vivo and in vivo skin permeation studies in rat using iontophoresis and chemical enhancers, J Con Rel.2003 ;89:127-140.
Hitendra SM, Saurabh KS, Sanjay J, Surana J. Nasal in-situ gel containing hydroxy propyl β-cyclodextrin inclusion complex of Artemether: Development and in-vitro evaluation. Incl Phenom Macrocycl Chem 2011; 70: 49.
Avinash BA, Pranit R, Ashwini B, Nitin M, Sanjay C. Formulation and evaluation of Eletriptan hydrobromide thermoreversible nasal in-situ gel. Int J Pharm Res Dev 2012; 4: 264-275.
Abhirami M, Brindha R, Optimization of in-situ gelling system for nasal administration of celecoxib. J Chem Pharm Res.2014; 6(2):502-515.
Nerelle A, Dontha P. Formulation and evaluation of in-situ mucoadhesive nasal gel of Montelukast sodium. Pelagia research library.Der Pharmcia Sinica.2014;5(2):1-8.
Parekh HB, Rishad J, Jivani NP, Patel LD, Ami M, Krunal S. Novel in-situ polymeric drug delivery system: a review. J Drug Del Ther. 2012; 2(5): 136-145.
Patel RP, Baria AH, Pandya NB, Tank HM. Formulation Evaluation and optimization Of stomach specific in situ gel of Ranitidine hydrochloride. Int J Pharm Sci Nanotech. 2010; 3(1): 834-843.
Rubinstein A., Friend D.R, Specific delivery to the gastrointestinal tract, in: Domb A.J (Ed.), Polymeric Site-Specific Pharmacotherapy, Wiley, Chichester, 1994, 282-283.
Whitehead L.., .Fell J., Sharma H.L. Floating dosage forms: an in vivo study demonstrating prolonged gastric retention. J.cont. Rel. 1998,55:3-12
Ichikawa M, Watanabe S, Miyake Y. A new multiple unit oral floating dosage system. I: Preparation and in vitro evaluation of floating and sustained release kinetics. Pharm Sci.1991; 80:1062- 1066.
Innuccelli V, Coppi G, Bernabei M T, Cameroni R. Air compartment multipleunit system for prolonged gastric residence. Int J Pharm.1998; 174:47-54.
Goole J, Vanderbist F, Aruighi K. Development and Evaluation of new multiple-unit Levodopa sustained release floating dosage forms. Int J Pharm 2007:334:35-41.
Sharma S, Pawar A. Low density multiparticulate system for pulasatile release of Meloxicam. Int J Pharm 2006:313:150-58.
Jamini M and Joshi V. Floating Multiparticulate Oral Drug Delivery System: A Review. Int Res J Pharmacy. 2013; 3(12):59-50.
Semalty M. Preparation and characterization of floating microspheres of ofloxacin hydrochloride. Int J Pharm Sci Nanotech. 2010; 4(1):819-823.
Sato Y., Kawashima Y. Physicochemical properties to determine the buoyancy of hollow
microspheres (microballoons) prepared by the emulsion solvent diffusion method. Eur J Pharm Sci. 2003,55:297-304
Ikura, Hiroshi, Suzuki, Yoshiki United States Patent 4777033.1988
Umezawa, Hamao United States Patent 4101650.1978
Thanoo B.C, Sunny M.C. and Jayakrishnan A., Oral sustained-release drug delivery systems using polycarbonate microspheres capable of floating on the gastric fluid, J Pharm Pharmacol. 1993,45,21-24.
Sato Y., Kawashima Y., Takeuchi H. and Yamamoto H., In vivo evaluation of riboflavin containing microballoons for floating controlled drug delivery system in healthy human volunteers, J Cont Rel 2003, 93, 39-47
Joseph NH, Laxmi S, Jayakrishnan A. A floating type oral dosage form for piroxicam based on hollow microspheres: in vitro and in vivo evaluation in rabbits. J Cont Rel. 2002; 79:71-79.
Thanoo BC, Sunny MC, Jayakrishnan A. Oral sustained release drug delivery systems using polycarbonate microspheres capable of floating on the gastric fluids. J Pharm Pharmacol.1993; 45:21-24.
Rajnikanth P, Mishra B. Floating in situ gelling system for stomach site specific delivery of clarithromycin to eradicate H.pylori. J Cont Rel. 2008; 25:33-41
Itoh K, Hatakeyama T, Shimoyama T, Miyazaki S, D’Emanuele A, Attwood D. In situ gelling formulation based on methylcellulose/pectin system for oral-sustained drug delivery to dysphagic patients. Drug Dev Indus Pharmacy. 2011; 37(7): 790–797
He C, Kim SW, Lee DS. In situ gelling stimuli-sensitive block copolymer hydrogels for drug delivery. J Con Rel. 2008; 127:189–207.
Singh NK, Lee DS, In-situ gelling pH and temperature sensitive biodegradable block copolymer hydrogels for drug delivery. J Cont Rel. 2014;
http://dx.dio.org/10.1016/j.jconrel/2014.04.056.
Thilek KM, Bharathi D, Balasubramaniam J, Kant S, Pandit JK. pH-induced in-situ gelling systems of Indomethacin for sustained ocular delivery. Indian J Pharm Sci 2005; 67(3): 327-333.
Jivani RR, Patel CN, Jivani NP. The influence of variation of gastric pH on the gelation and release characteristics of in situ gelling sodium alginate formulations. Acta Pharma Sciencia. 2010; 52: 365-369
Srividya B, Cardoza RM, Amin. Sustained ophthalmic delivery of Ofloxacin from a pH triggered in-situ gelling system. J Con Rel 2001; 73: 205-211.
Swati G, Suresh PV. Carbopol/Chitosan based pH triggered in-situ gelling system for ocular delivery of Timolol Maleate. Scientia Pharmaceutia 2010; 78(4): 959–976.
Shi-lei CAO, Qi-zhi Z, Xin-guo J. Preparation of ion-activated in-situ gel systems of Scopolamine hydrobromide and evaluation of its antimotion sickness efficacy. Acta Pharmacol Sin 2007; 28(4): 584–590.
Wang S, Chen P, Zhang L, Yang C, Zhai G. Formulation and evaluation of microemulsion-based in-situ ion-sensitive gelling systems for intranasal administration of Curcumin. J Drug Targeting 2012; 20: 831-840.
Bhalerao KK, Kamble MS et al. A short review on stomach specific floating in-situ gel. J Biomed Pharm Res.2012; 1(3):1-4.
Nirmal HB, Bakliwal S, Pawar SP. In-Situ gel: New trends in Controlled and Sustained Drug Delivery System. Int J Pharm Tech Res 2010; 2: 1398-1408
Radi Hejazi, Mansoor Amiji. Chitosan based gastrointestinal delivery systems. J Cont Rel 2013:89:151- 165.
Miyazaki S, Endo K., Kawasaki N, Kubo W, Watanabe H, Attwood D. Oral sustained delivery of Paracetamol from in-situ gelling xyloglucan formulations. Drug Dev Ind Pharm 2003; 29(2): 113-119
Nerkar TS, Gujrathi NA. In-situ gel: A novel approach in sustained and controlled drug delivery system. Int J Pharm Sci. 2013; 4(4):1-18.
Shinde S, Tadwee I, Shahi S. Gastroretentive drug delivery system: A review. Int J Pharm Res All Sci. 2012;1(1): 1-13.
Pande SD. Floating drug delivery system (FDDS): A new way for oral drug delivery system. Int J Pharm Clinical Sci. 2013;3(1): 1-13.
