Enhancement of Solubility BCS Class II and IV Pharmaceuticals by Liqusolid Technique: A review
Abstract
Many techniques can be used to improve drug solubility, which is the development of the liquisolid technique. This technique has a mechanism for increasing the surface area of the drug as well as wetting from the addition of non-volatile solvents resulting in a lower surface tension and contact angle, so the solubility and drug release very increases. Liquisolid tablets show a lower contact angle compared to the conventional tablets. The liquisolid technique approach is also promising because the process is simple in making low production costs and allows the manufacturing industry, including non-volatile solvents, fillers, dryers, and disintegrants. Liquisolid characterized by specific instruments such as powder x-ray diffraction (PXRD), Fourier transforms infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and scanning electron microscope (SEM). Several liquisolid techniques are described in this review. The liquisolid technique is proven and able to change the physicochemical properties of active pharmaceutical ingredients, especially the solubility, drug release, and stability of the formula so that this technique can be a solution for class II and IV BCS pharmaceutical active drug classes.
Keywords: Active Pharmaceutical Ingredients, Contact Angle, Solubility, Drug Release, Stability, Liquisolid Technique
References
Ghadi R, Dand N. BCS class IV drugs: Highly notorious candidates for formulation development. J Control Release [Internet]. 2017;248:71–95. Available from: http://dx.doi.org/10.1016/j.jconrel.2017.01.014
Gad SC, Cassidy CD, Aubert N, Spainhour B, Robbe H. Nonclinical vehicle use in studies by multiple routes in multiple species. Int J Toxicol. 2006;25(6):499–521.
Strickley RG. Solubilizing excipients used in commercially available oral and injectable formulations. Pharm Res. 2004;21(2):201–30.
Barzegar-Jalali M, Dastmalchi S. Kinetic Analysis of Chlorpropamide Dissolution from Solid Dispersions. Drug Dev Ind Pharm. 2007;98(411):63–70.
Barzegar-Jalali M, Valizadeh H, Shadbad M-RS, Adibkia K, Mohammadi G, Farahani A, et al. Cogrinding as an approach to enhance dissolution rate of a poorly water-soluble drug ( gliclazide ). Powder Technol [Internet]. 2010;197(3):150–8. Available from: http://dx.doi.org/10.1016/j.powtec.2009.09.008
Ma K, Wang N, Cheng L, Wei Y, Zhang J, Gao Y. Identification of novel adefovir dipivoxil-saccharin cocrystal polymorphs and their thermodynamic polymorphic transformations. Int J Pharm [Internet]. 2019;566(May):361–70. Available from: https://doi.org/10.1016/j.ijpharm.2019.05.071
Patel B, Shah C. Recent research on liquisolid technology for solubility enhancement-A review. Int J Adv Pharm. 2016;345–94.
Vasconcelos T, Sarmento B, Costa P. Solid dispersions as strategy to improve oral bioavailability of poor water soluble drugs. Drug Discov Today. 2007;12(23/24):1068–75.
Wang X, Michoel A, Den V, Mooter G. Solid state characteristics of ternary solid dispersions composed of PVP VA64, Myrj 52 and itraconazole. Int J Pharm. 2005;303(1–2):54–61.
Shah VP, Amidon GP. G.L. Amidon, H. Lennernas, V.P. Shah, and J.R. Crison. A Theoretical Basis for a Biopharmaceutic Drug Classification: The Correlation of In Vitro Drug Product Dissolution and In Vivo Bioavailability, Pharm Res 12, 413–420, 1995—Backstory of BCS [Internet]. Vol. 16, The AAPS Journal. 2014. Available from: http://link.springer.com/10.1208/s12248-014-9620-9
El-Sayyad NME-M, Badawi A, Abdullah ME, Abdelmalak NS. Dissolution enhancement of leflunomide incorporating self emulsifying drug delivery systems and liquisolid concepts. Bull Fac Pharmacy, Cairo Univ [Internet]. 2017; Available from: http://dx.doi.org/10.1016/j.bfopcu.2017.02.001
Spireas. Liquisolid System and Methods of Preparing Same. United States Pat. 2002;1(12):1–9.
Khaled KA, Asiri YA, El-sayed YM. In vivo evaluation of hydrochlorothiazide liquisolid tablets in beagle dogs. Int J Pharm. 2001;222:1–6.
Yadav VB, Yadav A V. Improvement of Solubility and Dissolution of Indomethacin by Liquisolid and Compaction Granulation Technique. J Pharm Sci Res. 2009;1(2):44–51.
Hentzschel C., Alnaief M, Smirnova I, Sakmann A, Leopold C. Enhancement of griseofulvin release from liquisolid compacts. Eur J Pharm Biopharm. 2012;80(1):130–5.
Sharma V, Pathak K. Attempts and outcomes of liquisolid technology: An updated chronological compilation of innovative ideas and adjuvants in the field. Pharm Biomed Res. 2016;2(15):1–21.
Javadzadeh Y, Siahi MR, Asnaashari S, Nokhodchi A. An investigation of physicochemical properties of piroxicam liquisolid compacts. Pharm Dev Technol. 2007;12(3):337–43.
Javadzadeh Y, Siahi-Shadbad M., Barzegar-Jalali, Nokhodchi A. Enhancement of dissolution rate of piroxicam using liquisolid compacts. Farm. 2005;60:361–5.
Javadzadeh Y, Jafari-navimipour B, Nokhodchi A. Liquisolid technique for dissolution rate enhancement of a high dose water-insoluble drug ( carbamazepine ). Int Jorunal Pharm. 2007;341:26–34.
Nokhodchi A, Hentzschel CM, Leopold CS. Drug Release From Liquisolid Systems: Speed it up, Slow it down. Int J Pharm Sci Nanotechnol [Internet]. 2010;3(1):795–802. Available from: http://www.tandfonline.com/doi/full/10.1517/17425247.2011.548801
Khan A, Agrawal S. Formulation and Evaluation of Lumefantrine Capsule Prepared by Using Liquisolid Technique. Int J Curr Pharm Res. 2018;10(2):43–50.
Savkare A, Bhavsar M, VD G, Kukar P. Liquisolid Technique : A Review. Int J Pharm Pharm Sci. 2017;8:68–75.
Kulkarni AS, Aloorkar NH, Mane MS, Gaja JB. Liquisolid Systems : A Review. Intertional J Pharm Sci Nanotechnol. 2010;3(1):795–802.
Sharma G, Khatry S, Arora S. Formulation and characterization of liquisolid compacts of valsartan. J Pharm Res. 2012;5(8):4158–62.
Bonthagarala B, Dasari V, KOtra V, Swain S, Beg S. Quality-by-Design based development and characterization of pioglitazone loaded liquisolid compact tablets with improved biopharmaceutical attributes [Internet]. Vol. 51, Journal of Drug Delivery Science and Technology. Elsevier B.V.; 2019. 345–355 p. Available from: https://doi.org/10.1016/j.jddst.2019.03.033
Chopra DK, Madhab DK, Sahu PK. Improvement of Oral Bioavailability of Azilsartan Medoxomil By Lipid Based Liquisolid Compacts: in Vitro and in Vivo Evaluation. Int Res J Pharm. 2019;9(12):134–9.
Naveen C, Shastri N, Tadikonda RR. Use of the liquisolid compact technique for improvement of the dissolution rate of valsartan. Acta Pharm Sin B [Internet]. 2012;2(5):502–8. Available from: https://linkinghub.elsevier.com/retrieve/pii/S2211383512001165
Dias RJ, Ranjan S, Mali KK, Ghorpade VS, Havaldar VD. Liquisolid Compacts of Meloxicam : in-vitro and in-vivo evaluation. Egypt Pharm J. 2018;190–200.
Yehia SA, El-Ridi MS, Tadros MI, El-Sherif NG. Enhancement of the oral bioavailability of fexofenadine hydrochloride via cremophor® el-based liquisolid tablets. Adv Pharm Bull [Internet]. 2015;5(4):569–81. Available from: http://dx.doi.org/10.15171/apb.2015.077
Tiong N, Elkordy AA. Effects of liquisolid formulations on dissolution of naproxen. Eur J Pharm Biopharm [Internet]. 2009;73(3):373–84. Available from: http://dx.doi.org/10.1016/j.ejpb.2009.08.002
Komala DR, Janga KY, Jukanti R, Bandari S, Vijayagopal M. Competence of raloxifene hydrochloride loaded liquisolid compacts for improved dissolution and intestinal permeation. J Drug Deliv Sci Technol [Internet]. 2015;30:232–41. Available from: http://dx.doi.org/10.1016/j.jddst.2015.10.020
Nagabandi V, Tadikonda R, N. JK. Formulation Development and Evaluation of Liquisolid Systems To Improve the Dissolution Rate of Ketoprofen. Int J Biomed Res. 2012;2(10):3667–72.
Elkordy AA, Essa EA, Dhuppad S, Jammigumpula P. Liquisolid technique to enhance and to sustain griseofulvin dissolution: Effect of choice of non-volatile liquid vehicles. Int J Pharm [Internet]. 2012;434(1–2):122–32. Available from: http://dx.doi.org/10.1016/j.ijpharm.2012.05.072
Javadzadeh Y, Musaalrezaei L, Nokhodchi A. Liquisolid technique as a new approach to sustain propranolol hydrochloride release from tablet matrices. Int J Pharm. 2008;362:102–8.
Hassan M., El-saghir H. Enhancement of Dissolution and the Antiinflammatory Effect of Nimesulide, using Liquisolid Compact for Oral Application. Bull Pharm Sci,. 2011;34:1–8.
Scrivens G, Ticehurst M, Swanson JT. Strategies for Improving the Reliability of Accelerated Predictive Stability (APS) Studies [Internet]. Accelerated Predictive Stability. Elsevier Inc.; 2018. 175–206 p. Available from: http://dx.doi.org/10.1016/B978-0-12-802786-8.00007-3
Sanka K, Poienti S, Mohd AB, Diwan P V. Improved oral delivery of clonazepam through liquisolid powder compact formulations : In-vitro and ex-vivo characterization. Powder Technol [Internet]. 2014;256:336–44. Available from: http://dx.doi.org/10.1016/j.powtec.2014.02.026
Berthomieu C, Heinerwadel R. Fourier transform infrared ( FTIR ) spectroscopy. Photosynth Res. 2009;101:157–70.
Sayyad FJ, Tulsankar SL, Kolap UB. Design and development of liquisolid compact of candesartan cilexetil to enhance dissolution. J Pharm Res [Internet]. 2013 May;7(5):381–8. Available from: http://dx.doi.org/10.1016/j.jopr.2013.05.012
Gong Y, Grant DJW, Brittain HG. Principles of Solubility. 1995;
Muthyala J, Singh SK, Gulati M, Kumar B, Rathee H, Ghai D, et al. Systematic development and characterization of liquisolid compacts of atorvastatin-glipizide binary mixture to achieve enhanced dissolution and stability profile. Asian J Pharm. 2016;10(4).
Harsha INS, Lohithasu D, Babu KM, Madhu G, Lavanya K, Swaroop KK. Formulation and Characterization of Piroxicam Liquisolid Technique for Solubility Enhancement. 2014;3(3):1393–404.
Reddy KV, Reddy D., Shruti P. Principles of Drug Release In Various Dosage Forms. World J Pharm Res. 2015;3(April):4.
Akinlade B, Elkordy AA, Essa EA, Elhagar S. Liquisolid systems to improve the dissolution of Furosemide. Sci Pharm. 2010;78(2):325–44.
Srinivas L, Kumar V, Ramya P, Manasa P. Preparation and biopharmaceutical evaluation of piroxicam liquisolid system. INDO Am J Pharm Sci. 2014;
Jain R, Brito L, Straub J. Effect of powder processing on perfomance of Fenofibrate formulations. Eur J Biopharm. 2008;69(34):727.
Huang Q, Wang J, Zang Z-B. Preparation of ultrafine Fenofibrate powder by solidification process from emulsion. Int J Pharm. 2008;368:160–4.
Vogt M, Kunath K, Dressman J. Dissolution enhancement of Fenofibrate by micronization, co-grinding and spray-drying comparison with commercial preparations. Eur J Pharm Biopharm. 2008;68:283–8.
Refbacks
- There are currently no refbacks.