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Design and development of sodium alginate/ carboxymethyl cellulose in situ gelling system for gastroretentive delivery of lisinopril

Yıl 2023, Cilt: 27 Sayı: 2, 825 - 836, 27.06.2025

Kiran Patil , Jyoti Patil Sneha Bharade John Disouza Ashok Hajare

Öz

Lisinopril is a potent ACE (angiotensin-converting enzyme) inhibitor used to treat hypertension and
congestive heart failure. It exhibits 25% of low bioavailability. Hence, in the current study, the major objective was to
increase the gastric transient time of lisinopril and develop in situ gel formulation for better absorption and modulating
release behavior of lisinopril. Different formulations of lisinopril were prepared by using gelling polymers such as
Carboxymethyl cellulose (CMC), pectin, and calcium carbonate. Sodium citrate was used to prevent gelation outside
the gastric environment. The formulation was studied using Fourier Transform Infrared Spectroscopy (FTIR) and
Differential Scanning Calorimetry (DSC) to interpret the interaction between drugsand polymers. For optimization of
in situ gelling system 32 full factorial design was employed to study the effect of independent variables, the
concentration of CMC (X1) and concentration of sodium alginate (X2), on the dependent variables viscosity, and % drug
content. Formulation (F5) containing 1.25% of sodium alginate, and 0.75% of CMC showed good gelling ability. The
composition F5 was optimized on the basis of viscosity (5.03 Pa.s), drug content (94.06±1.0%), and cumulative drug
release (95±0.73%) at 12 h. Floating in situ gelling system improved bioavailability and gastric transit time of lisinopril.
A stability study indicated the absence of any noticeable change in the formulation. Thus, in situ gel formulation is a
promising approach for gastro-retentive sustained delivery of lisinopril. These results ensure that the developed system
is an alternative to conventional drug delivery systems and can enhance patient compliance.

Anahtar Kelimeler

In situ Gel Sodium Alginate Carboxymethyl cellulose Gastro-retentive drug delivery Lisinopril

Kaynakça

  • Hypertension- WHO. https://www.who.int/news-room/fact-sheets/detail/hypertension (accessed on 25 August 2021)
  • High blood pressure - adults - MedlinePlus. https://medlineplus.gov/ency/article/000468.htm. (accessed on 27 January 2020)
  • Pant S, Badola A, Kothiyal P. A review on gastro retentive drug delivery system. Int J of Res Dev Pharm Life Sci. 2016; 5(4): 2178-2187.
  • Tripathi J, Thapa P, Maharjan R, Jeong SH. Current State and Future Perspectives on Gastroretentive Drug Delivery Systems. Pharmaceutics. 2019;11(4):193. [CrossRef]
  • Timmermans J, Moes AJ. How Well Floating Dosage Form Float?. Int J Pharm. 1990;62:207‐216.[CrossRef]
  • Strebeul A, Siepmann J, Bodmeier R. Gastro retentive drug delivery system. Expert Opin Drug Deliv. 2006; 3(2): 217-33. [CrossRef]
  • Bardonnet PL, Faivre V, Pugh WJ, Piffaretti JC, Falson F. Gastroretentive dosage forms: overview and a special case of Helicobacter pylori. J Control Release. 2006; 111(1-2): 1-18. [CrossRef]
  • Pawar VK, Kansal S, Garg G, Awasthi R, Singodia D, Kulkarni GT, Gastroretentive dosage forms: A review with special emphasis on floating drug delivery systems. Drug Delivery. 2011;18(2):97-110.[CrossRef]
  • Nayak AK, Maji R, Das B. Gastroretentive drug delivery system: A review. Asian J Pharm Clin Res. 2010;3(1):1-10.
  • Cheien YW. Novel drug delivery system (2nd ed). New York, Marcell Dekker Inc., 1999:1-42.
  • Brahmankar DM, Jaiswal SB. Biopharmaceutics and pharmacokinetics, Vallabh Prakashan. New Delhi; 335-370.
  • Miyazaki S, Endo K, Kawasaki N, Kubo W, Watanabe H, Attwood D. Oral sustained delivery of paracetamol from in situ gelling xyloglucan formulations. Drug DevIndPharma. 2003;29(2):113-119. [CrossRef]
  • Palepu S, Sathyanarayana T, Ravali M, Dakshyani P, Ubbala S, Pathipati D S, Madupalli S. Preparation and evaluation of fast dissolving sublingual film of lisinopril. J Drug Deliv Ther. 2019; 9(1-s): 101-106. [CrossRef]
  • Lancaster SG, Todd PA. Lisinopril: A preliminary review of its pharmacodynamic and pharmacokinetic properties and therapeutic use in hypertension and congestive heart failure. Drugs. 1988; 35: 646-669. [CrossRef]
  • Gupta R, Mishra AK, Pathak AK. A critical review on different pharmaceutical aspects of solid dispersion technique for solubility enhancement. Int J Pharm Bio Sci. 2015; 5(3): 119–128.
  • Kumari K, Sharma P, Gupta R. Polysorbate-Phospholipid Complex Micelles as P-glycoprotein Inhibitor Drug Delivery System. J Basic Pharmacol Toxicol. 2017; 1(1): 2-7.
  • Akash Tandon, Pankaj Kumar Jangra. Formulation and in vitro Evaluation of Lisinopril floating Gastroretentive Tablets. Research J. Pharm. and Tech. 2021; 14(1):207-213. [CrossRef]
  • Shimoyama T, Itoh K, Kobayashi M, Miyazaki S, D’Emanuele A, Attwood D. Oral liquid in situ gelling methylcellulose/alginate formulations for sustained drug delivery to dysphagic patients. Drug Dev. Ind. Pharm. 2012. 38:8, 952-960. [CrossRef]
  • Jankovic A, Chaudhary G, Goia F.Designing the design of experiments (DOE) – An investigation on the influence of different factorial designs on the characterization of complex systems. Energy & Buildings. 2021; 250:111298. [CrossRef]
  • Ranga S, Jaimini M, Sharma SK, Singh Chauhan B, Kumar A. A Review on Design of Experiments (DOE). Int. j. pharm. chem. sci. 2014; 3(1):216-20.
  • Sangeetha S, Harish G, Medapati R, Gantasala P, Bomma R, Damodharan N. Oral sustained delivery of salbutamol using in-situ gelation of sodium alginate. Int J of Curr Pharm Res. 2010; 2(3): 61-64.
  • Seddiqi H, Oliaei E, Honarkar H, Jin J, Geonzon LC, Bacabac RG, Klein-Nulend. Cellulose and its derivatives: towards biomedical applications. Cellulose. 2021;28:1893-1931. [CrossRef]
  • Hajare A, Dol H, Patil k. Design and development of terbinafine hydrochloride ethosomal gel for enhancement of transdermal delivery: In vitro, in vivo, molecular docking, and stability study, J. Drug Deliv. Sci. Technol. 2021; 61:102280. [CrossRef]
  • Gherrak F, Abdelkader H, Lefnaoui S. Implementation and in vitro characterization of calcium-free in situ gelling oral reconstituted suspension for potential overweight treatment. Drug Dev. Ind. Pharm. 2020;47(1):36-50. [CrossRef]
  • Tarek AA, Bader MA. A potential in situ gel formulation loaded with novel fabricate poly(lactide-co-glycolide) nanoparticles for enhancing & sustaining the ophthalmic delivery of ketoconazole. Int J of Nanomedicine. 2017;12:1863-75.[CrossRef]
  • Panwar AS, Sharma M, Optimization and evaluation of famotidine In situ gel using two level three factor full factorial design. Inventi Rapid:NDDS. 2014. 2014(4):1-5.
  • Patil KS, Hajare AA, Manjappa AS, More HN, Disouza JI. Design, development, in silico, and in vitro characterization of Docetaxel-loaded TPGS/ Pluronic F 108 mixed micelles for improved cancer treatment. J Drug Deliv Sci. Technol. 2021; 65: 102685. [CrossRef]
  • De Anjan, Chakraborty S, Mukherjee A, Chattopadhyay J, Ghatak S. Design and optimization of nasal in situ gel of Ondansetron using factorial design. Int jres in pharm chem. 2013;3(3):659-674.
  • Madan JR, Adokar BR, Dua K. Development and evaluation of in situ gel of pregabalin. Int J Pharm Investig.015;5(4):226-233.[CrossRef]
  • Maheswaran A, Padmavathy J, Nandhını V, Saravanan D, Angel P. Formulation and evaluation of floating oral in situ gel of diltiazem hydrochloride. Int J App Pharm. 2017;9(1):50-5. [CrossRef]
  • Statistically designed novel ranolazine-loaded ethosomal transdermal gel for the treatment of angina pectoris HS Dol, AA Hajare, KS Patil Journal of Drug Del. Sci. and Tech. 75, 103574, 2022.[CrossRef]
  • Chaniyara S, Modi D, Patel R, Patel J, Desai R, Chaudhary S.Formulation and evaluation of floatable in situ gel for stomach-specific delivery of ofloxacin. Am J Adv Drug Deliv. 2013;1(3):285-299.
  • Hajare AA, Velapure PD, Rathod PN, Patil KS, Chopade SS. Formulatıon and evaluatıon of solıd lıpıd nanopartıcle gel for topıcal delıvery of clobetasol propıonate to enhance ıts permeatıon usıng sılk serıcın as permeatıon enhancer. Int J Pharm Sci Res. 2020; 11(5): 2356-2365.[CrossRef]
  • Shastri DH, Dodiya HD, Shelat P, Bhanupriy AK. Formulation Development and Evaluation of Gastroretentivein situ oral gel of Cefuroxime Axetil. J Young Pharm. 2016; 8(4): 324-329. [CrossRef]
  • Khan S, Gajbhiye C, Singhavi DJ, Yeole P. In situ gel of metoprolol tartrate: Physicochemical characterization, In vitro diffusion and histological studies. Indian J Pharm Sci, 2012, 74 (6): 564-570. [CrossRef]
  • Sindhoor SM, Priya S, Maxwell A. Formulation and evaluation of novel in situ gel of Lafutidine for gastroretentive drug delivery. Asian J Pharm Clin Res. 2018; 11(8): 88-94. [CrossRef]
  • Pandya K, Agrawal P, Dashora A, Sahu D, Garg R, Pareta L, Menaria M, Joshi B. Formulation and evaluation of oral floatable in situ gel of Ranitidine hydrochloride. J Drug Deliv. Ther. 2013, 3(3): 90-97. [CrossRef]
  • Bhatta RG, Rudragangaiah S, Kotappa SBB. Formulation, Optimization, and Evaluation of in situ Gelling Liquid Oral Formulation of a Novel Antidiabetic Drug: Canagliflozin. Indian J Pharm Educ Res. 2019; 53(2S): s121-s128. [CrossRef]
  • Sharma A, Sharma J, Kaur R, Saini V. Development and characterization of in situ oral gel of Spiramycin. BioMed Res Int. 2014; 876182: 1-7. [CrossRef]
  • Pashikanti S, Jyothsna B.Formulation and evaluation of floating in situ gel of ciprofloxacin, Int. J. Appl. Pharm. 2019;11(1), 198–204. [CrossRef]
  • Sanjana A, Ahmed MG, JaswanthGowda BH. Preparation and evaluation of in situ gels containing hydrocortisone for the treatment of aphthous ulcer. J. Oral Biol. Craniofacial Res. 2021;11:269–276. [CrossRef]
  • Ahmed MG, Kapoor C, Adinarayana S. Formulation and evaluation of oral sustained in situ gelling system of Roxatidine. Indonesian J Pharm. 2017; 28(3): 179-184. [CrossRef]
  • Jayswal BD, Yadav VT, Patel KN, Patel BA, Patel PA. Formulation and evaluation of floating in situ gel based gastro retentive drug delivery of Cemetidine. Int J Pharm Res Scholars. 2012; 1(2): 327-337.

Yıl 2023, Cilt: 27 Sayı: 2, 825 - 836, 27.06.2025

Kiran Patil , Jyoti Patil Sneha Bharade John Disouza Ashok Hajare

Öz

Kaynakça

  • Hypertension- WHO. https://www.who.int/news-room/fact-sheets/detail/hypertension (accessed on 25 August 2021)
  • High blood pressure - adults - MedlinePlus. https://medlineplus.gov/ency/article/000468.htm. (accessed on 27 January 2020)
  • Pant S, Badola A, Kothiyal P. A review on gastro retentive drug delivery system. Int J of Res Dev Pharm Life Sci. 2016; 5(4): 2178-2187.
  • Tripathi J, Thapa P, Maharjan R, Jeong SH. Current State and Future Perspectives on Gastroretentive Drug Delivery Systems. Pharmaceutics. 2019;11(4):193. [CrossRef]
  • Timmermans J, Moes AJ. How Well Floating Dosage Form Float?. Int J Pharm. 1990;62:207‐216.[CrossRef]
  • Strebeul A, Siepmann J, Bodmeier R. Gastro retentive drug delivery system. Expert Opin Drug Deliv. 2006; 3(2): 217-33. [CrossRef]
  • Bardonnet PL, Faivre V, Pugh WJ, Piffaretti JC, Falson F. Gastroretentive dosage forms: overview and a special case of Helicobacter pylori. J Control Release. 2006; 111(1-2): 1-18. [CrossRef]
  • Pawar VK, Kansal S, Garg G, Awasthi R, Singodia D, Kulkarni GT, Gastroretentive dosage forms: A review with special emphasis on floating drug delivery systems. Drug Delivery. 2011;18(2):97-110.[CrossRef]
  • Nayak AK, Maji R, Das B. Gastroretentive drug delivery system: A review. Asian J Pharm Clin Res. 2010;3(1):1-10.
  • Cheien YW. Novel drug delivery system (2nd ed). New York, Marcell Dekker Inc., 1999:1-42.
  • Brahmankar DM, Jaiswal SB. Biopharmaceutics and pharmacokinetics, Vallabh Prakashan. New Delhi; 335-370.
  • Miyazaki S, Endo K, Kawasaki N, Kubo W, Watanabe H, Attwood D. Oral sustained delivery of paracetamol from in situ gelling xyloglucan formulations. Drug DevIndPharma. 2003;29(2):113-119. [CrossRef]
  • Palepu S, Sathyanarayana T, Ravali M, Dakshyani P, Ubbala S, Pathipati D S, Madupalli S. Preparation and evaluation of fast dissolving sublingual film of lisinopril. J Drug Deliv Ther. 2019; 9(1-s): 101-106. [CrossRef]
  • Lancaster SG, Todd PA. Lisinopril: A preliminary review of its pharmacodynamic and pharmacokinetic properties and therapeutic use in hypertension and congestive heart failure. Drugs. 1988; 35: 646-669. [CrossRef]
  • Gupta R, Mishra AK, Pathak AK. A critical review on different pharmaceutical aspects of solid dispersion technique for solubility enhancement. Int J Pharm Bio Sci. 2015; 5(3): 119–128.
  • Kumari K, Sharma P, Gupta R. Polysorbate-Phospholipid Complex Micelles as P-glycoprotein Inhibitor Drug Delivery System. J Basic Pharmacol Toxicol. 2017; 1(1): 2-7.
  • Akash Tandon, Pankaj Kumar Jangra. Formulation and in vitro Evaluation of Lisinopril floating Gastroretentive Tablets. Research J. Pharm. and Tech. 2021; 14(1):207-213. [CrossRef]
  • Shimoyama T, Itoh K, Kobayashi M, Miyazaki S, D’Emanuele A, Attwood D. Oral liquid in situ gelling methylcellulose/alginate formulations for sustained drug delivery to dysphagic patients. Drug Dev. Ind. Pharm. 2012. 38:8, 952-960. [CrossRef]
  • Jankovic A, Chaudhary G, Goia F.Designing the design of experiments (DOE) – An investigation on the influence of different factorial designs on the characterization of complex systems. Energy & Buildings. 2021; 250:111298. [CrossRef]
  • Ranga S, Jaimini M, Sharma SK, Singh Chauhan B, Kumar A. A Review on Design of Experiments (DOE). Int. j. pharm. chem. sci. 2014; 3(1):216-20.
  • Sangeetha S, Harish G, Medapati R, Gantasala P, Bomma R, Damodharan N. Oral sustained delivery of salbutamol using in-situ gelation of sodium alginate. Int J of Curr Pharm Res. 2010; 2(3): 61-64.
  • Seddiqi H, Oliaei E, Honarkar H, Jin J, Geonzon LC, Bacabac RG, Klein-Nulend. Cellulose and its derivatives: towards biomedical applications. Cellulose. 2021;28:1893-1931. [CrossRef]
  • Hajare A, Dol H, Patil k. Design and development of terbinafine hydrochloride ethosomal gel for enhancement of transdermal delivery: In vitro, in vivo, molecular docking, and stability study, J. Drug Deliv. Sci. Technol. 2021; 61:102280. [CrossRef]
  • Gherrak F, Abdelkader H, Lefnaoui S. Implementation and in vitro characterization of calcium-free in situ gelling oral reconstituted suspension for potential overweight treatment. Drug Dev. Ind. Pharm. 2020;47(1):36-50. [CrossRef]
  • Tarek AA, Bader MA. A potential in situ gel formulation loaded with novel fabricate poly(lactide-co-glycolide) nanoparticles for enhancing & sustaining the ophthalmic delivery of ketoconazole. Int J of Nanomedicine. 2017;12:1863-75.[CrossRef]
  • Panwar AS, Sharma M, Optimization and evaluation of famotidine In situ gel using two level three factor full factorial design. Inventi Rapid:NDDS. 2014. 2014(4):1-5.
  • Patil KS, Hajare AA, Manjappa AS, More HN, Disouza JI. Design, development, in silico, and in vitro characterization of Docetaxel-loaded TPGS/ Pluronic F 108 mixed micelles for improved cancer treatment. J Drug Deliv Sci. Technol. 2021; 65: 102685. [CrossRef]
  • De Anjan, Chakraborty S, Mukherjee A, Chattopadhyay J, Ghatak S. Design and optimization of nasal in situ gel of Ondansetron using factorial design. Int jres in pharm chem. 2013;3(3):659-674.
  • Madan JR, Adokar BR, Dua K. Development and evaluation of in situ gel of pregabalin. Int J Pharm Investig.015;5(4):226-233.[CrossRef]
  • Maheswaran A, Padmavathy J, Nandhını V, Saravanan D, Angel P. Formulation and evaluation of floating oral in situ gel of diltiazem hydrochloride. Int J App Pharm. 2017;9(1):50-5. [CrossRef]
  • Statistically designed novel ranolazine-loaded ethosomal transdermal gel for the treatment of angina pectoris HS Dol, AA Hajare, KS Patil Journal of Drug Del. Sci. and Tech. 75, 103574, 2022.[CrossRef]
  • Chaniyara S, Modi D, Patel R, Patel J, Desai R, Chaudhary S.Formulation and evaluation of floatable in situ gel for stomach-specific delivery of ofloxacin. Am J Adv Drug Deliv. 2013;1(3):285-299.
  • Hajare AA, Velapure PD, Rathod PN, Patil KS, Chopade SS. Formulatıon and evaluatıon of solıd lıpıd nanopartıcle gel for topıcal delıvery of clobetasol propıonate to enhance ıts permeatıon usıng sılk serıcın as permeatıon enhancer. Int J Pharm Sci Res. 2020; 11(5): 2356-2365.[CrossRef]
  • Shastri DH, Dodiya HD, Shelat P, Bhanupriy AK. Formulation Development and Evaluation of Gastroretentivein situ oral gel of Cefuroxime Axetil. J Young Pharm. 2016; 8(4): 324-329. [CrossRef]
  • Khan S, Gajbhiye C, Singhavi DJ, Yeole P. In situ gel of metoprolol tartrate: Physicochemical characterization, In vitro diffusion and histological studies. Indian J Pharm Sci, 2012, 74 (6): 564-570. [CrossRef]
  • Sindhoor SM, Priya S, Maxwell A. Formulation and evaluation of novel in situ gel of Lafutidine for gastroretentive drug delivery. Asian J Pharm Clin Res. 2018; 11(8): 88-94. [CrossRef]
  • Pandya K, Agrawal P, Dashora A, Sahu D, Garg R, Pareta L, Menaria M, Joshi B. Formulation and evaluation of oral floatable in situ gel of Ranitidine hydrochloride. J Drug Deliv. Ther. 2013, 3(3): 90-97. [CrossRef]
  • Bhatta RG, Rudragangaiah S, Kotappa SBB. Formulation, Optimization, and Evaluation of in situ Gelling Liquid Oral Formulation of a Novel Antidiabetic Drug: Canagliflozin. Indian J Pharm Educ Res. 2019; 53(2S): s121-s128. [CrossRef]
  • Sharma A, Sharma J, Kaur R, Saini V. Development and characterization of in situ oral gel of Spiramycin. BioMed Res Int. 2014; 876182: 1-7. [CrossRef]
  • Pashikanti S, Jyothsna B.Formulation and evaluation of floating in situ gel of ciprofloxacin, Int. J. Appl. Pharm. 2019;11(1), 198–204. [CrossRef]
  • Sanjana A, Ahmed MG, JaswanthGowda BH. Preparation and evaluation of in situ gels containing hydrocortisone for the treatment of aphthous ulcer. J. Oral Biol. Craniofacial Res. 2021;11:269–276. [CrossRef]
  • Ahmed MG, Kapoor C, Adinarayana S. Formulation and evaluation of oral sustained in situ gelling system of Roxatidine. Indonesian J Pharm. 2017; 28(3): 179-184. [CrossRef]
  • Jayswal BD, Yadav VT, Patel KN, Patel BA, Patel PA. Formulation and evaluation of floating in situ gel based gastro retentive drug delivery of Cemetidine. Int J Pharm Res Scholars. 2012; 1(2): 327-337.
Toplam 43 adet kaynakça vardır.

Ayrıntılar

Birincil Dil İngilizce
Konular Eczacılık ve İlaç Bilimleri (Diğer)
Bölüm Articles
Yazarlar

Kiran Patil 0000-0002-3248-6063

Jyoti Patil 0000-0003-1899-6945

Sneha Bharade 0000-0002-8754-8102

John Disouza 0000-0002-9807-7932

Ashok Hajare

Yayımlanma Tarihi 27 Haziran 2025
Yayımlandığı Sayı Yıl 2023 Cilt: 27 Sayı: 2

Kaynak Göster

APA Patil, K., Patil, J., Bharade, S., Disouza, J., vd. (2025). Design and development of sodium alginate/ carboxymethyl cellulose in situ gelling system for gastroretentive delivery of lisinopril. Journal of Research in Pharmacy, 27(2), 825-836.
AMA Patil K, Patil J, Bharade S, Disouza J, Hajare A. Design and development of sodium alginate/ carboxymethyl cellulose in situ gelling system for gastroretentive delivery of lisinopril. J. Res. Pharm. Haziran 2025;27(2):825-836.
Chicago Patil, Kiran, Jyoti Patil, Sneha Bharade, John Disouza, ve Ashok Hajare. “Design and Development of Sodium Alginate/ Carboxymethyl Cellulose in Situ Gelling System for Gastroretentive Delivery of Lisinopril”. Journal of Research in Pharmacy 27, sy. 2 (Haziran 2025): 825-36.
EndNote Patil K, Patil J, Bharade S, Disouza J, Hajare A (01 Haziran 2025) Design and development of sodium alginate/ carboxymethyl cellulose in situ gelling system for gastroretentive delivery of lisinopril. Journal of Research in Pharmacy 27 2 825–836.
IEEE K. Patil, J. Patil, S. Bharade, J. Disouza, ve A. Hajare, “Design and development of sodium alginate/ carboxymethyl cellulose in situ gelling system for gastroretentive delivery of lisinopril”, J. Res. Pharm., c. 27, sy. 2, ss. 825–836, 2025.
ISNAD Patil, Kiran vd. “Design and Development of Sodium Alginate/ Carboxymethyl Cellulose in Situ Gelling System for Gastroretentive Delivery of Lisinopril”. Journal of Research in Pharmacy 27/2 (Haziran 2025), 825-836.
JAMA Patil K, Patil J, Bharade S, Disouza J, Hajare A. Design and development of sodium alginate/ carboxymethyl cellulose in situ gelling system for gastroretentive delivery of lisinopril. J. Res. Pharm. 2025;27:825–836.
MLA Patil, Kiran vd. “Design and Development of Sodium Alginate/ Carboxymethyl Cellulose in Situ Gelling System for Gastroretentive Delivery of Lisinopril”. Journal of Research in Pharmacy, c. 27, sy. 2, 2025, ss. 825-36.
Vancouver Patil K, Patil J, Bharade S, Disouza J, Hajare A. Design and development of sodium alginate/ carboxymethyl cellulose in situ gelling system for gastroretentive delivery of lisinopril. J. Res. Pharm. 2025;27(2):825-36.