LOPERAMIDE LOADED POLYMERIC NANOSPONGES FOR ENHANCED BIOAVAILABILITY: FORMULATION DEVELOPMENT AND IN-VITRO EVALUATION
Main Article Content
Keywords
Anti-diarrheal, nanosponges, pharmaceutical technology, cyclodextrin based nanosponges, loperamide HCl
Abstract
Loperamide HCl belongs to antidiarrheals group used for the treatment of variety of acute, chronic or traveler’s diarrhea by slowing down an overactive bowel leading to the decreased number of bowel movements. This study involved loperamide loaded beta cyclodextrin-based nano sponges that were found to be effective for treating diarrhea. Beta-Cyclodextrin, polyvinyl alcohol and dimethylsulfoxide are employed to fabricate nanosponges through emulsion solvent diffusion technology with little modifications. Antidiarrheal drug loperamide HCl loaded beta cyclodextrin based nano sponges were formulated and evaluated for studying physiochemical characteristics. Fourier Transform Infrared spectroscopy and scanning electron microscopy were used for structural analysis. Drug compatibility with excipients used in the formulation was determined by FTIR analysis. The development of inclusion complexes with porous and spherical morphology was verified by FTIR without any chemical interaction between drug and polymer. Spherical, spongy, porous and nano sized three-dimensional structure was shown by scanning electron microscopy. Analysis of particle size, percent yield, drug loading and entrapment efficiency of nano sponges were also performed. The particle size of formulation was in nano size range. The percentage yield was in the range of 91 and 94%. The entrapment effectiveness and percent drug loading were between 89% and 90%. In the in-vitro release experiment, loperamide loaded beta cyclodextrin based nanosponge formulations revealed continuous drug release profile with the absence of burst release phenomenon. The findings of all the studies confirmed that encapsulation of drug in nanosponges led to improvement in its efficacy in terms of its solubility, dissolution , release and therapeutic applications.
References
2. Koirala S, Nepal P, Ghimire G, Basnet R, Rawat I, Dahal A. Formulation and evaluation of mucoadhesive buccal tablets of aceclofenac. Heliyon [Internet]. 2021 Mar 1 [cited 2023 Apr 11];7(3):e06439. Available from: https://linkinghub.elsevier.com/retrieve/pii/S2405844021005442
3. Rashid M, Ahmad QZ, Tajuddin. Trends in Nanotechnology for Practical Applications. In: Applications of Targeted Nano Drugs and Delivery Systems: Nanoscience and Nanotechnology in Drug Delivery. Elsevier; 2019. p. 297–325.
4. Blanco E, Shen H, Ferrari M. Principles of nanoparticle design for overcoming biological barriers to drug delivery. Nat Biotechnol [Internet]. 2015 Sep 1 [cited 2024 May 15];33(9):941–51. Available from: https://www.nature.com/articles/nbt.3330
5. Jain A, Prajapati SK, Kumari A, Mody N, Bajpai M. Engineered nanosponges as versatile biodegradable carriers: An insight. J Drug Deliv Sci Technol. 2020 Jun 1;57:101643.
6. Rajam RP, Muthukumar KR. An updated comprehensive review on nanosponges – novel emerging drug delivery system. Res J Pharm Technol. 2021 Aug 1;14(8):4476–84.
7. Agrawal R V, Gangurde RB, Jadhav KR. NANOSPONGES: AN OVERVIEW ON PROCESSING, APPLICATION AND EVALUATION. World J Pharm Res [Internet]. 2020 [cited 2024 May 15];9(12):273–87. Available from: www.wjpr.net
8. Shoaib QUA, Abbas N, Irfan M, Hussain A, Arshad MS, Hussain SZ, et al. Development and evaluation of scaffold-based nanosponge formulation for controlled drug delivery of naproxen and ibuprofen. Trop J Pharm Res [Internet]. 2018 Oct 5 [cited 2024 May 14];17(8):1465–74. Available from: https://www.ajol.info/index.php/tjpr/article/view/178153
9. Rao MRP, Chaudhari J, Trotta F, Caldera F. Investigation of Cyclodextrin-Based Nanosponges for Solubility and Bioavailability Enhancement of Rilpivirine. AAPS PharmSciTech [Internet]. 2018 Jul 1 [cited 2024 May 14];19(5):2358–69. Available from: https://link.springer.com/article/10.1208/s12249-018-1064-6
10. Le TAT, Nguyen BT, Kim MH, Kim B, Kim HS, Jeong SW, et al. Development of official assay method for loperamide hydrochloride capsules by HPLC. Anal Sci Technol. 2020 Dec 1;33(6):252–61.
11. MacDonald R, Heiner J, Villarreal J, Strote J. Loperamide dependence and abuse. Case Reports [Internet]. 2015 May 2 [cited 2024 May 15];2015. Available from: https://casereports.bmj.com/content/2015/bcr-2015-209705
12. Loos NHC, Bui V, de Jong DH, Lebre MC, Rosing H, Beijnen JH, et al. Impact of loperamide on the pharmacokinetics and tissue disposition of ritonavir-boosted oral docetaxel therapy; a preclinical assessment. Cancer Chemother Pharmacol [Internet]. 2024 Mar 8 [cited 2024 May 15];1–9. Available from: https://link.springer.com/article/10.1007/s00280-024-04662-8
13. Kumar A, Rao R. Enhancing efficacy and safety of azelaic acid via encapsulation in cyclodextrin nanosponges: development, characterization and evaluation. Polym Bull [Internet]. 2021 Sep 1 [cited 2024 May 14];78(9):5275–302. Available from: https://link.springer.com/article/10.1007/s00289-020-03366-2
14. Penjuri SCB, Ravouru N, Damineni S, Bns S, Poreddy SR, Yüklü Nanosüngerlerin Formülasyonu ve Değerlendirilmesi L. Formulation and Evaluation of Lansoprazole Loaded Nanosponges. Turk J Pharm Sci. 2016;13(3):304–10.
15. Allahyari S, Esmailnezhad N, Valizadeh H, Ghorbani M, Jelvehgari M, Ghazi F, et al. In-vitro characterization and cytotoxicity study of flutamide loaded cyclodextrin nanosponges. J Drug Deliv Sci Technol. 2021 Feb 1;61:102275.
16. Zewail MB, F.Asaad G, Swellam SM, Abd-allah SM, K.Hosny S, Sallah SK. Design, characterization and in vivo performance of solid lipid nanoparticles (SLNs)-loaded mucoadhesive buccal tablets for efficient delivery of Lornoxicam in experimental inflammation. Int J Pharm. 2022 Aug 25;624:122006.
17. Ullah S, Azad AK, Nawaz A, Shah KU, Iqbal M, Albadrani GM. 5-Fluorouracil-Loaded Folic-Acid-Fabricated Chitosan Nanoparticles for Site-Targeted Drug Delivery Cargo. Polymers (Basel) [Internet]. 2022 May 13 [cited 2023 May 3];14(10):2010. Available from: https://www.mdpi.com/2073-4360/14/10/2010/htm
18. Jafri I, Shoaib MH, Yousuf RI, Ali FR. Effect of permeation enhancers on in vitro release and transdermal delivery of lamotrigine from Eudragit®RS100 polymer matrix-type drug in adhesive patches. Prog Biomater [Internet]. 2019 Jun 1 [cited 2022 Jun 26];8(2):91–100. Available from: https://link.springer.com/article/10.1007/s40204-019-0114-9
19. Sobhani H, Tarighi P, Ostad SN, Shafaati A, Nafissi-Varcheh N, Aboofazeli R. Rapamycin-Loaded, CapryolTM 90 and Oleic Acid Mediated Nanoemulsions: Formulation Development, Characterization and Toxicity Assessment. Iran J Pharm Res [Internet]. 2018 [cited 2022 Oct 13];17(3):830–50. Available from: /pmc/articles/PMC6094419/
20. Chen X ting, Wang T. Preparation and characterization of atrazine-loaded biodegradable PLGA nanospheres. J Integr Agric. 2019 May 1;18(5):1035–41.
21. Allahou LW, Madani SY, Seifalian A. Investigating the Application of Liposomes as Drug Delivery Systems for the Diagnosis and Treatment of Cancer. Int J Biomater. 2021;1–16.
22. Altaani BM, Almaaytah AM, Dadou S, Alkhamis K, Daradka MH, Hananeh W. Oral Delivery of Teriparatide Using a Nanoemulsion System: Design, in Vitro and in Vivo Evaluation. Pharm Res [Internet]. 2020 Apr 1 [cited 2021 Dec 26];37(4):1–15. Available from: https://link.springer.com/article/10.1007/s11095-020-02793-0
23. Alejandro B, Guillermo T, Ángeles PM. Formulation and Evaluation of Loperamide HCl Oro Dispersible Tablets. Pharmaceuticals [Internet]. 2020 May 18 [cited 2024 May 15];13(5):100. Available from: https://www.mdpi.com/1424-8247/13/5/100/htm
24. Alvarado JG, Quilaqueo M, Hermosilla J, González S, Medina C, Rolleri A, et al. Degree of crosslinking in β-cyclodextrin-based nanosponges and their effect on piperine encapsulation. Food Chem. 2021 Mar 15;340:128132.
25. Jang JH, Jeong SH, Lee YB. Preparation and In Vitro/In Vivo Characterization of Polymeric Nanoparticles Containing Methotrexate to Improve Lymphatic Delivery. Int J Mol Sci [Internet]. 2019 Jul 5 [cited 2023 Jan 29];20(13):3312. Available from: https://www.mdpi.com/1422-0067/20/13/3312/htm
26. Šahinović M, Hassan A, Kristó K, Regdon G, Vranić E, Sovány T. Quality by Design-Based Development of Solid Self-Emulsifying Drug Delivery System (SEDDS) as a Potential Carrier for Oral Delivery of Lysozyme. Pharmaceutics [Internet]. 2023 Mar 1 [cited 2024 Feb 21];15(3):995. Available from: https://www.mdpi.com/1999-4923/15/3/995/htm
27. Pilicheva B, Uzunova Y, Marudova M. Polyelectrolyte Multilayer Films as a Potential Buccal Platform for Drug Delivery. Polymers (Basel) [Internet]. 2022 Feb 14 [cited 2023 Apr 11];14(4):734. Available from: https://www.mdpi.com/2073-4360/14/4/734/htm
28. Nitish, Jeganath S, Abdelmagid KFK. A Review on Nanosponges – A Promising Novel Drug Delivery System. Res J Pharm Technol. 2021 Jan 1;14(1):501–5.
29. Gad S, Alhussini S, Gardouh AR. Polymeric nano sponge drug delivery system: A review. Rec Pharm Biomed Sci [Internet]. 2022 Apr 1 [cited 2024 May 14];6(3):34–58. Available from: https://rpbs.journals.ekb.eg/article_231964.html
30. Ghurghure SM, Sana M, Pathan A, Surwase R. Nanosponges: A novel approach for targeted drug delivery system. Int J Chem Stud [Internet]. 2018 [cited 2024 May 14];2(6):15–23. Available from: www.chemistryjournal.in
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Rimsha Liaqat
Punjab University College of Pharmacy, University of the Punjab, Lahore, Pakistan, Allama Iqbal Campus, Lahore 54000
Pervaiz Akhtar Shah
Punjab University College of Pharmacy, University of the Punjab, Lahore, Pakistan, Allama Iqbal Campus, Lahore 54000
Hashmat Ullah
Gomal Centre of Pharmaceutical Sciences, Faculty of Pharmacy, Gomal University, Dera Ismail Khan, 29050, Pakistan
Syed Atif Raza
Punjab University College of Pharmacy, University of the Punjab, Lahore, Pakistan, Allama Iqbal Campus, Lahore 54000
Sheikh Abdur Rashid
Gomal Centre of Pharmaceutical Sciences, Faculty of Pharmacy, Gomal University, Dera Ismail Khan, 29050, Pakistan
Farwa Shaheen
Punjab University College of Pharmacy, University of the Punjab, Lahore, Pakistan, Allama Iqbal Campus, Lahore 54000
Saima Mahmood
Gomal Centre of Pharmaceutical Sciences, Faculty of Pharmacy, Gomal University, Dera Ismail Khan, 29050, Pakistan
Afifa Tariq
Punjab University College of Pharmacy, University of the Punjab, Lahore, Pakistan, Allama Iqbal Campus, Lahore 54000
Mobina Manzoor
Lahore College for Women University
Ghulam Mustafa Khan
Department of Chemistry, University of Balochistan, Quetta
Sidra Mumtaz
Gomal Centre of Pharmaceutical Sciences, Faculty of Pharmacy, Gomal University, Dera Ismail Khan, 29050, Pakistan
Afaq Babar
Gomal Centre of Pharmaceutical Sciences, Faculty of Pharmacy, Gomal University, Dera Ismail Khan, 29050, Pakistan