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Current Materials Science

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ISSN (Print): 2666-1454
ISSN (Online): 2666-1462

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Research Article

Quality by Design Enabled β-Cyclodextrin Complexes of Lisinopril by Kneading Method: Improved Solubility and Bioavailability

Author(s): Azeez Mohammad*, Sumer Singh, Suryakanta Swain and Debashish Ghose

Volume 17, Issue 2, 2024

Published on: 04 May, 2023

Page: [135 - 147] Pages: 13

DOI: 10.2174/2666145416666230407100318

Price: $65

Abstract

Background: The primary intent of the study is to formulate the inclusion complex of lisinopril with the varied compositions of polymers like β-cyclodextrin for the enhancement of oral drug solubility and bioavailability using QbD approach.

Methods: The application of Box-behnken design to determine the optimized run from the prepared inclusion complexes. The physical kneading technique with β-cyclodextrin at varied amounts was used to create the inclusion complex of lisinopril.

Results: The FT-IR analysis study confirmed the selected drug, polymers, and other excipients showed no physical interactions. The prepared inclusion complexes' particle sizes and encapsulation efficiency were between 802 to 3259μm, 19.22 to 93.28%. The optimized formulation batch (F5) showed 90.16% in vitro drug release at 24h compared to the pure drug. From the in vivo study, the pharmacokinetic parameters for the optimized formulation (F5) were found to be Cmax of 94.336 ng/ml, Tmax of 12h, and AUC 94.336 ng.h/ml, Kel of 0.0395h-1 and t1/2 of 12h. After three months, stability studies for the optimized formulation batch indicate no change in drug entrapment efficiency and other parameters.

Conclusion: The β-cyclodextrin inclusion complex of lisinopril exhibited a 2-fold increase in the oral bioavailability of the model drug, which will be the novel drug-delivery strategy for the treatment of hypertension.

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[1]
Desai PM, Er PXH, Liew CV, Heng PWS. Functionality of disintegrants and their mixtures in enabling fast disintegration of tablets by a quality by design approach. AAPS PharmSciTech 2014; 15(5): 1093-104.
[http://dx.doi.org/10.1208/s12249-014-0137-4] [PMID: 24848762]
[2]
Brewster ME, Loftsson T. Cyclodextrins as pharmaceutical solubilizers. Adv Drug Deliv Rev 2007; 59(7): 645-66.
[http://dx.doi.org/10.1016/j.addr.2007.05.012] [PMID: 17601630]
[3]
Kurkov SV, Loftsson T. Cyclodextrins. Int J Pharm 2013; 453(1): 167-80.
[http://dx.doi.org/10.1016/j.ijpharm.2012.06.055] [PMID: 22771733]
[4]
Ferrari R, Guardigli G, Mele D, Valgimigli M, Ceconi C. Myocardial ischaemia: New evidence for angiotensin-converting enzyme inhibition. Eur Heart J Suppl 2003; 5: E11-7.
[http://dx.doi.org/10.1016/S1520-765X(03)90027-7]
[5]
Job P. Formation and stability of inorganic complexes in solution. Ann Chim 1928; 9: 113-203.
[6]
Szejtli J. Past, present and futute of cyclodextrin research. Pure Appl Chem 2004; 76(10): 1825-45.
[http://dx.doi.org/10.1351/pac200476101825]
[7]
Salústio PJ, Feio G, Figueirinhas JL, Pinto JF, Cabral Marques HM. The influence of the preparation methods on the inclusion of model drugs in a β-cyclodextrin cavity. Eur J Pharm Biopharm 2009; 71(2): 377-86.
[http://dx.doi.org/10.1016/j.ejpb.2008.09.027] [PMID: 18977436]
[8]
Torricelli C, Martini A, Muggetti L, Eli M, De Ponti R. Stability studies on steroidal drug/β-cyclodextrin kneaded systems. Int J Pharm 1991; 75(2-3): 147-53.
[http://dx.doi.org/10.1016/0378-5173(91)90188-T]
[9]
Das S, Subuddhi U. Studies on the complexation of diclofenac sodium with β–cyclodextrin: Influence of method of preparation. J Mol Struct 2015; 1099: 482-9.
[http://dx.doi.org/10.1016/j.molstruc.2015.07.001]
[10]
Gil A, Chamayou A, Leverd E, Bougaret J, Baron M, Couarraze G. Evolution of the interaction of a new chemical entity, eflucimibe, with γ-cyclodextrin during kneading process. Eur J Pharm Sci 2004; 23(2): 123-9.
[http://dx.doi.org/10.1016/j.ejps.2004.06.002] [PMID: 15451000]
[11]
Olaru A, Borodi G, Kacsó I, Vasilescu M, Bratu I, Cozar O. Spectroscopic studies of the inclusion compound of lisinopril with β -cyclodextrin. Spectroscopy 2009; 23(3-4): 191-9.
[http://dx.doi.org/10.1155/2009/837158]
[12]
Bratu I, Kacso I, Borodi G, Constantinescu DE, Dragan F. Inclusion compound of Fosinopril with β -cyclodextrin. Spectroscopy 2009; 23(1): 51-8.
[http://dx.doi.org/10.1155/2009/275398]
[13]
Prabhu S, Ortega M, Ma C. Novel lipid-based formulations enhancing the in vitro dissolution and permeability characteristics of a poorly water-soluble model drug, piroxicam. Int J Pharm 2005; 301(1-2): 209-16.
[http://dx.doi.org/10.1016/j.ijpharm.2005.05.032] [PMID: 16046087]
[14]
Pamudji JS, Mauludin R, Lestari VA. Improvement of carvedilol dissolution rate through formation of inclusion complex with β-cyclodextrin. Int J Pharm Pharm Sci 2014; 6: 228-33.
[15]
Sherje AP, Kulkarni V, Murahari M, et al. Inclusion complexation of etodolac with hydroxypropyl-beta-cyclodextrin and auxiliary agents: Formulation characterization and molecular modeling studies. Mol Pharm 2017; 14(4): 1231-42.
[http://dx.doi.org/10.1021/acs.molpharmaceut.6b01115] [PMID: 28248111]
[16]
Derle D, Bele M, Kasliwal N. In vitro and in vivo evaluation of mefenamic acid and its complexes with β-Cyclodextrin and HP-β-Cyclodextrin. Asian J Pharm 2008; 2(1): 30-4.
[http://dx.doi.org/10.4103/0973-8398.41562]
[17]
Bulani VD, Kothavade PS, Kundaikar HS, et al. Inclusion complex of ellagic acid with β-cyclodextrin: Characterization and in vitro anti-inflammatory evaluation. J Mol Struct 2016; 1105: 308-15.
[http://dx.doi.org/10.1016/j.molstruc.2015.08.054]
[18]
Fateminasab F, Bordbar AK, Shityakov S, Gholami S. Diadzein complexation with unmodified cyclodextrins: A detailed experimental and theoretical study. J Mol Liq 2018; 271: 80-95.
[http://dx.doi.org/10.1016/j.molliq.2018.08.124]
[19]
Khoukhi OE, El Bahri Z, Diaf K, Baitiche M. Piroxicam/β-cyclodextrin complex included in cellulose derivatives-based matrix microspheres as new solid dispersion-controlled release formulations. Chem Pap 2016; 70(6): 828-39.
[http://dx.doi.org/10.1515/chempap-2016-0014]
[20]
Hirlekar RS, Sonawane SN, Kadam VJ. Studies on the effect of water-soluble polymers on drug-cyclodextrin complex solubility. AAPS PharmSciTech 2009; 10(3): 858-63.
[http://dx.doi.org/10.1208/s12249-009-9274-6] [PMID: 19562489]
[21]
Siva S, Kothai Nayaki S, Rajendiran N. Spectral and molecular modeling investigations of supramolecular complexes of mefenamic acid and aceclofenac with α- and β-cyclodextrin. Spectrochim Acta A Mol Biomol Spectrosc 2017; 174: 349-62.
[http://dx.doi.org/10.1016/j.saa.2014.12.002] [PMID: 29941144]
[22]
Pradines B, Gallard JF, Iorga BI, et al. Investigation of the complexation of albendazole with cyclodextrins for the design of new antiparasitic formulations. Carbohydr Res 2014; 398: 50-5.
[http://dx.doi.org/10.1016/j.carres.2014.06.008] [PMID: 25240182]
[23]
Rudrangi SRS, Bhomia R, Trivedi V, et al. Influence of the preparation method on the physicochemical properties of indomethacin and methyl-β-cyclodextrin complexes. Int J Pharm 2015; 479(2): 381-90.
[http://dx.doi.org/10.1016/j.ijpharm.2015.01.010] [PMID: 25579867]
[24]
Bernardi LS, Oliveira PR, Murakami FS, Silva MAS, Borgmann SHM, Cardoso SG. Characterization of venlafaxine hydrochloride and compatibility studies with pharmaceutical excipients. J Therm Anal Calorim 2009; 97(2): 729-33.
[http://dx.doi.org/10.1007/s10973-009-0282-2]
[25]
Liu L, Zhu S. Preparation and characterization of inclusion complexes of prazosin hydrochloride with β-cyclodextrin and hydroxypropyl-β-cyclodextrin. J Pharm Biomed Anal 2006; 40(1): 122-7.
[http://dx.doi.org/10.1016/j.jpba.2005.06.022] [PMID: 16095859]
[26]
Sreenivasa RK, Udgirkar DB, Mule DD. Enhancement of dissolution rate and bioavailability of aceclofenac by complexation with cyclodextrin. RJPBCS 2010; 1: 142-51.
[27]
Swain S, Behera UA, Beg S, et al. Design and characterization of enteric-coated controlled release mucoadhesive microcapsules of Rabeprazole sodium. Drug Dev Ind Pharm 2013; 39(4): 548-60.
[http://dx.doi.org/10.3109/03639045.2012.676047] [PMID: 22512732]
[28]
Swain S, Behera A, Dinda SC, et al. Formulation design, optimization, and pharmacodynamic evaluation of sustained release mucoadhesive microcapsules of venlafaxine HCl. Indian J Pharm Sci 2014; 76(4): 354-63.
[PMID: 25284934]
[29]
Swain S, Patra CN, Sruti J, Rao MEB. Design and evaluation of sustained-release solid dispersions of verapamil hydrochloride. Int J Pharm Sci Nanotech 2011; 3(4): 1252-62.
[30]
Lin HL, Lin SY, Lin CC, Hsu CH, Wu TK, Huang YT. Mechanical grinding effect on thermodynamics and inclusion efficiency of loratadine-cyclodextrin inclusion complex formation. Carbohydr Polym 2012; 87(1): 512-7.
[http://dx.doi.org/10.1016/j.carbpol.2011.08.010] [PMID: 34662996]
[31]
Aigner Z, Berkesi O, Farkas G, Szabó-Révész P. DSC, X-ray and FTIR studies of a gemfibrozil/dimethyl-β-cyclodextrin inclusion complex produced by co-grinding. J Pharm Biomed Anal 2012; 57: 62-7.
[http://dx.doi.org/10.1016/j.jpba.2011.08.034] [PMID: 21920691]
[32]
Gascon AR, Cuadrado A, Solinís MA, et al. Comparative bioavailability of two immediate-release tablets of lisinopril/hydrochlorothiazide in healthy volunteers. Int J Clin Pharmacol Ther 2003; 41(7): 309-15.
[http://dx.doi.org/10.5414/CPP41309] [PMID: 12875347]
[33]
Eyjolfsson R. Lisinopril-lactose incompatibility. Drug Dev Ind Pharm 1998; 24(8): 797-8.
[http://dx.doi.org/10.3109/03639049809082729] [PMID: 9876529]

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