Formulation Development and Evaluation of Sustained Release Ranolazine Microbeads using Natural Polymer
Abstract
The goal of this study was to develop sustained-release microbeads containing Ranolazine. The Ranolazine was selected on the basis of its short half-life i.e., 1.5 h and used in treatment of Angina pectoris. The fundamental goal of this research is to increase duration of drug release. Ranolazine was encapsulated with natural polymers such as Hygrophila auriculata seed mucilage by an ionotropic gelation technique. The formulation batches were optimized with a 32 factorial design and physicochemical characteristics were also evaluated. The particle size of microbeads, entrapment efficiency of drug, surface morphology, In-vitro release of drug was investigated.
The in-vitro studies of optimized microbeads formulation batch (B2) containing 100:600 ratio of Hygrophila auriculata seed mucilage and sodium alginate exhibited as a sustained release of Ranolazine up to 12 h and. The mucoadhesion potential was found to be 97± 1% up 12 h. In our perspective, the current ER pellet formulation might be the most feasible alternative to traditional pain management formulas.
All the trial’s batches were shown to be suitable in extended release of a short elimination half-life medication with enhanced bioavailability, implying that it is useful for oral drug delivery.
Keywords: Design of experiment, Extrusion-spheronization, Ionic gelation, Microbeads, Ranolazine,
Keywords:
Design of experiment, Extrusion-spheronization, Ionic gelation, Microbeads, RanolazineDOI
https://doi.org/10.22270/jddt.v13i4.5795References
Mathias NR, Hussain MA. Non-invasive systemic drug delivery: developability considerations for alternate routes of administration. Journal of Pharmaceutical Sciences. 2010; 99(1):1-20 https://doi.org/10.1002/jps.21793
Alqahtani MS, Kazi M, Alsenaidy MA, Ahmad MZ. Advances in oral drug delivery. Frontier in Pharmacology. 2021; 12: 1-21. https://doi.org/10.3389/fphar.2021.618411
Talevi A, Oral drug delivery. In: The ADME Encyclopedia: a comprehensive guide on biopharmacy and pharmacokinetics. Springer International Publishing, Cham; 2021. p.1-8. https://doi.org/10.1007/978-3-030-51519-5_11-1
Bhargava A, Rathore RPS, Tanwar YS, Gupta S, Bhaduka G, Oral sustained release dosage form: an opportunity to prolong the release of drug, International Journal of Advanced Research in Pharmaceutical and Bio Sciences, 2013; 2( 2):1-7.
Raut SY, Gahane A, Joshi MB, Kalthur G, Mutalik S, Nanocomposite clay-polymer microbeads for oral controlled drug delivery: Development and, in vitro and in vivo evaluations. Journal of Drug Delivery Science and Technology, 2019; 51:234-243. https://doi.org/10.1016/j.jddst.2019.03.001
Gaur PK, Mishra S, Bajpai M, Formulation and evaluation of controlled release of telmisartan microspheres: in vitro/in vivo study. Journal of Food and Drug Analysis, 2014; 22(4):542-548. https://doi.org/10.1016/j.jfda.2014.05.001
Dan N, Samanta K, Almoazen H, An update on pharmaceutical strategies for oral delivery of therapeutic peptides and proteins in adults and pediatrics, Children. 2020; 7(12)307:1-28. https://doi.org/10.3390/children7120307
Ramesh M, Rangappa SM, Parameswaranpillai J, Siengchin S, Introduction to biodegradable polymers, Ed. Rangappa SM Parameswaranpillai J, Siengchin S, Ramesh M, In: Biodegradable polymers, blends and composites. Woodhead Publishing; 2022. p.1-18. https://doi.org/10.1016/B978-0-12-823791-5.00024-7
Adepu S, Ramakrishna S. Controlled drug delivery systems: current status and future directions. Molecules. 2021; 26(19):5905. https://doi.org/10.3390/molecules26195905
Ummadi S, Shravani B, Rao NR, Reddy MS, Sanjeev B, Overview on controlled release dosage form System, International Journal of Pharma Sciences, 2013; 7(8):51-60.
Tiwari RK, Singh L, Sharma V, Alginate micro-beads in novel drug delivery system: an overview. International Journal of Pharmacy and Technology, 2013; 5(1):1-13.
Tiwari RK, Singh L, Sharma V, Alginate micro-beads in novel drug delivery system: an overview. International Journal of Pharmacy and Technology, 2013; 5(1):1-13.
Song R, Murphy M, Li C, Ting K, Soo C, Zheng Z. Current development of biodegradable polymeric materials for biomedical applications. Drug Design, Development and Theory, 2018; 24(12):3117-3145. https://doi.org/10.2147/DDDT.S165440
Schroeter J, Creating the framework for a widespread use of biodegradable polymers (standardization, labelling, legislation, biowaste management). Polymer Degradation and Stability, 1998; 59(1-3):377-381. https://doi.org/10.1016/S0141-3910(97)00203-6
Baveja SK, Rao KV, Arora J, Examination of natural gums and mucilages as sustaining materials in tablet dosage forms. Indian Journal of Pharmaceutical Sciences, 1988; 50(2):89-92.
Rubinstein A, Radai R, Ezra M, Pathak S, Rokem JS, In-vitro evaluation of calcium pectinate: a potential colon-specific drug delivery carrier. Pharmaceutical Research, 1993; 10(2):258-263. https://doi.org/10.1023/A:1018995029167
Odeku OA, Fell JT, Evaluation of khaya gum as a directly compressible matrix system for controlled release. Journal of Pharmacy and Pharmacology, 2004; 56(11):1365-1370. https://doi.org/10.1211/0022357044652
Chauhan NS, Dixit VK, Asteracantha longifolia (L.) Nees, Acanthaceae: chemistry, traditional, medicinal uses and its pharmacological activities-a review. Revista Brasileira de Farmacognosia, 2010; 20(5):812-817. https://doi.org/10.1590/S0102-695X2010005000022
Okunlola A, Odeku OA, Lamprecht A, Oyagbemi AA, Oridupa OA, Aina, OO, Design of cissus-alginate microbeads revealing mucoprotection properties in anti-inflammatory therapy. International Journal of Biological Macromolecules, 2015; 79:226-234. https://doi.org/10.1016/j.ijbiomac.2015.04.062
Marciniak TA, Serebruany V, Ranolazine, ACE Inhibitors, and Angiotensin Receptor Blockers. The American Journal of Medicine, 2019; 132(12): E844-E845. https://doi.org/10.1016/j.amjmed.2019.02.032
Cattaneo M, Porretta AP, Gallino A, Ranolazine: drug overview and possible role in primary microvascular angina management. International Journal of Cardiology, 2015; 181:376-381. https://doi.org/10.1016/j.ijcard.2014.12.055
Banerjee K, Ghosh RK, Kamatam S, Banerjee A, Gupta A, Role of Ranolazine in cardiovascular disease and diabetes: Exploring beyond angina. International Journal of Cardiology, 2017; 227:556-564. https://doi.org/10.1016/j.ijcard.2016.10.102
Deore UV, Mahajan HS, Isolation and characterization of natural polysaccharide from Cassia Obtustifolia seed mucilage as film forming material for drug delivery. International Journal of Biological Macromolecules, 2018; 115:1071-1078. https://doi.org/10.1016/j.ijbiomac.2018.04.174
Kaewmanee T, Bagnasco L, Benjakul S, Lanteri S, Morelli CF, Speranza G, Cosulich, ME, Characterisation of mucilages extracted from seven Italian cultivars of flax. Food Chemistry, 2014; 148:60-69. https://doi.org/10.1016/j.foodchem.2013.10.022
Choudhary PD, Pawar HA. Recently Investigated Natural Gums and Mucilages as Pharmaceutical Excipients: An Overview. J Pharm (Cairo). 2014; 2014:1-9. https://doi.org/10.1155/2014/204849
Gawale D, Sonawane RO, Pandey VV, Ige PP. Formulation and in-vitro characterization of multiple unit sustained release matrix pellets of lornoxicam using natural gumsIndian J Novel Drug Deliv 2013; 5(4): 208-220.
Mallappa MK, Kesarla R Banakar S, Calcium alginate-neusilin US2 nanocomposite microbeads for oral sustained drug delivery of poor water soluble drug aceclofenac sodium. Journal of drug delivery, 2015; 2015:1-14. https://doi.org/10.1155/2015/826981
Rajmohan D, Bellmer D, Characterization of spirulina-alginate beads formed using ionic gelation. International Journal of Food Science, 2019; 2019:1-7. https://doi.org/10.1155/2019/7101279
Lotfipour F, Mirzaeei S Maghsoodi M, Preparation and characterization of alginate and psyllium beads containing Lactobacillus acidophilus. The Scientific World Journal, 2012; 2012:1-8 https://doi.org/10.1100/2012/680108
Upadhyay M, Adena SKR, Vardhan H, Yadav SK, Mishra B, Locust bean gum and sodium alginate based interpenetrating polymeric network microbeads encapsulating capecitabine: improved pharmacokinetics, cytotoxicity and in vivo antitumor activity. Materials Science and Engineering: C, 2019; 104: 1-13. https://doi.org/10.1016/j.msec.2019.109958
Sonawane RO, Patil SD, Fabrication and statistical optimization of starch-κ-carrageenan cross-linked hydrogel composite for extended-release pellets of zaltoprofen. International Journal of Biological Macromolecules, 2018; 120:.2324-2334. https://doi.org/10.1016/j.ijbiomac.2018.08.177
Sonawane RO, Patil SD, Gelatin-κ-carrageenan polyelectrolyte complex hydrogel compositions for the design and development of extended-release pellets. International Journal of Polymeric Materials and Polymeric Biomaterials, 2017; 66(16):812-823. https://doi.org/10.1080/00914037.2016.1276060
Published
Abstract Display: 681 
PDF Downloads: 641 PDF Downloads: 180 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
.