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Abstract

An innovative technique for medication delivery is the supersaturated drug delivery system, which uses the drug's supersaturated condition in the gut to increase the drug's bioavailability. Low bioavailability, when taken orally, is caused by weak bases decreasing solubility as pH rises. Some excipients were utilized to stop or postpone the precipitation that occurs when there is change in pH. The purpose of this study is to analyze SDDS with a focus on its prospects for the future and its current advancements. This review's objectives were to compile the most recent findings on supersaturated drug delivery systems (SDDS). The most recent developments in SDDS, including the formulation of characteristics, are thoroughly explored. This review paper aims to give a thorough understanding of the biopharmaceutical foundation of the supersaturated drug delivery system. Because of their higher solubility and enhanced saturation, supersaturated drug delivery systems improve drug absorption as well as its bioavailability. This reviews the scientific and technological advancements in systems.

Keywords

Supersaturation, Bioavailability, Solid dispersion, pH.

Reference

  1. Guzman, H.R., Tawa, M., Zhang, Z., Ratana banangkoon, P., Shaw, P., Gardner, C.R., Chen, H., Moreau, J.P., Almarsson, O., Remenar, J.F., 2007. Combined use of crystalline salt forms and precipitation inhibitors to improve oral absorption of celecoxib from solid oral formulations. J. Pharm. Sci. 96, 2686–2702.
  2. Fong SYK, Bauer-Brandl A, Brandl M. Oral bioavailability enhancement through supersaturation: an update and meta-analysis. Expert. Opin. Drug Deliv. 14(3), 403–426 (2017).
  3. Jackson MJ, Kestur US, Hussain MA, Taylor LS. Dissolution of danazol amorphous solid dispersions: supersaturation and phase behavior as a function of drug loading and polymer type. Mol. Pharmaceutics 13(1), 223–231 (2015).
  4. Indulkar AS, Mo H, Gao Y, Raina SA, Zhang GGZ, Taylor LS. Impact of micellar surfactant on supersaturation and insight into solubilization mechanisms in supersaturated solutions of atazanavir. Pharm. Res. 34(6), 1276–1295 (2017).
  5. Nguyen MH, Yu H, Kiew TY, Hadinoto K. Cost-effective alternative to nano-encapsulation: amorphous curcumin–chitosan nanoparticle complex exhibiting high payload and supersaturation generation. Eur. J. Pharm. Biopharm. 96, 1–10 (2015).
  6. Yu H, Xia D, Zhu Q, Zhu C, Chen D, Gan Y. Supersaturated polymeric micelles for oral cyclosporine A delivery. Eur. J. Pharm. Biopharm. 85(3, Part B), 1325–1336 (2013).
  7. Raghavan SL, Schuessel K, Davis A, Hadgraft J. Formation and stabilisation of triclosan colloidal suspensions using supersaturated systems. Int. J. Pharm. 261(1), 153–158 (2003).
  8. Thomas N, Holm R, Mullertz A, Rades T. ¨ In vitro and in vivo performance of novel supersaturated self-nanoemulsifying drug delivery systems (super-SNEDDS). J. Control. Rel. 160(1), 25–32 (2012).
  9. Modi S, Xiang T-X, Anderson BD. Enhanced active liposomal loading of a poorly soluble ionizable drug using supersaturated drug solutions. J. Control. Rel. 162(2), 330–339 (2012)
  10. Brouwers J, Brewster ME, Augustijns P. Supersaturating drug delivery systems: the answer to solubility-limited oral bioavailability? J. Pharm. Sci. 98(8), 2549–2572 (2009).
  11. Marghussian V. 1 - glass crystallization. In: Nano-Glass Ceramics. William Andrew Publishing, Oxford, UK, 1–62 (2015).
  12. Rodríguez-Hornedo N, Murphy D. (1999). Significance of controlling crystallization mechanisms and kinetics in pharmaceutical systems. J Pharm Sci, 88, 651–660.
  13. Dunitz JD, Bernstein J. (1995). Disappearing polymorphs. Acc Chem Res, 28, 193–200.
  14. Sangwal K. (2007). Additives and Crystallization Processes: From Fundamentals to Applications. Chichester: John Wiley & Sons.
  15. Guo S, Zhang L, Wang Z, Liu J. (2002). [Effects of conditioned medium derived from different keratinocytes on proliferation and collagen synthesis of hypertrophic scar fibroblasts]. Zhonghua Zheng Xing Wai Ke Za Zhi, 18, 83–85.
  16. Gao P, Akrami A, Alvarez F, Hu J, Li L, Ma C, Surapaneni S. (2009). Characterization and optimization of AMG 517 supersaturatable self-emulsifying drug delivery system (S-SEDDS) for improved oral absorption. J Pharm Sci, 98, 516–528.
  17. Raina, S. A.; Zhang, G. G.; Alonzo, D. E.; Wu, J.; Zhu, D.; Catron, N. D.; Gao, Y.; Taylor, L. S. Enhancements and limits in drug membrane transport using supersaturated solutions of poorly water-soluble drugs. J. Pharm. Sci. 2014, 103, (9), 2736-2748.
  18. Dai WG, Dong LC, Shi X, Nguyen J, Evans J, Xu Y, Creasey AA. (2007). Evaluation of drug precipitation of solubility-enhancing liquid formulations using milligram quantities of a new molecular entity (NME). J Pharm Sci, 96, 2957–2969.
  19. Jakubiak, P.; Wagner, B.; Grimm, H.P.; Petrig-Schaffland, J.; Schuler, F.; Alvarez-Sánchez, R. Development of a Unified Dissolution and Precipitation Model and Its Use for the Prediction of Oral Drug Absorption. Mol. Pharm. 2016, 13, 586–598.
  20. Osmani, R.A.M.; Hani, U.; Bhosale, R.R.; Kulkarni, P.K.; Shanmuganathan, S. Nanosponge Carriers—An Archetype Swing in Cancer Therapy: A Comprehensive Review. Curr. Drug Targets 2016, 18, 108–118.
  21. Krenn, L., Unterrieder, I., Ruprechter, R., 2002. Quantification of isoflavones in red clover by high-performance liquid chromatography. J. Chromatogr. B: Analyt. Technol. Biomed. Life Sci. 777, 123–128.
  22. Tsume, Y.; Matsui, K.; Searls, A.L.; Takeuchi, S.; Amidon, G.E.; Sun, D.; Amidon, G.L. The impact of supersaturation level for oral absorption of BCS class IIb drugs, dipyridamole and ketoconazole, using in vivo predictive dissolution system: Gastrointestinal Simulator (GIS). Eur. J. Pharm. Sci. 2017, 102, 126–139
  23. Jaisamut, P.; Wiwattanawongsa, K.; Graidist, P.; Sangsen, Y.; Wiwattanapatapee, R. Enhanced Oral Bioavailability of Curcumin Using a Supersaturatable Self-Micro Emulsifying System Incorporating a Hydrophilic Polymer; In Vitro and In Vivo Investigations. AAPS Pharm SciTech 2018, 19, 730–740.
  24. O’Shea, J.P.; Nagarsekar, K.; Wieber, A.; Witt, V.; Herbert, E.; O’Driscoll, C.M.; Saal, C.; Lubda, D.; Griffin, B.T.; Dressman, J.B. Mesoporous silica-based dosage forms improve bioavailability of poorly soluble drugs in pigs: Case example fenofibrate. J. Pharm. Pharmacol. 2017, 69, 1284–1292.
  25. Michaelsen, M.H.; Siqueira Jorgensen, S.D.; Abdi, I.M.; Wasan, K.M.; Rades, T.; Mullertz, A. Fenofibrate oral absorption from SNEDDS and super-SNEDDS is not significantly affected by lipase inhibition in rats. Eur. J. Pharm. Biopharm. 2019, 142, 258–264.
  26. Ruff, A.; Holm, R.; Kostewicz, E.S. Evaluating the predictability of the in vitro transfer model and in vivo rat studies as a surrogate to investigate the supersaturation and precipitation behavior of different Albendazole formulations for humans. Eur. J. Pharm. Sci. 2017, 105, 108–118.
  27. Tanaka, Y.; Sugihara, M.; Kawakami, A.; Imai, S.; Itou, T.; Murase, H.; Saiki, K.; Kasaoka, S.; Yoshikawa, H. In vivo analysis of supersaturation /precipitation /absorption behavior after oral administration of pioglitazone hydrochloride salt; determinant site of oral absorption. Eur. J. Pharm. Sci. 2017, 106, 431–438.
  28. Feng, D.; Peng, T.; Huang, Z.; Singh, V.; Shi, Y.; Wen, T.; Lu, M.; Quan, G.; Pan, X.; Wu, C. Polymer–Surfactant System Based Amorphous Solid Dispersion: Precipitation Inhibition and Bioavailability Enhancement of Itraconazole. Pharmaceutics 2018,10, 53.
  29. Suys, E.J.A.; Chalmers, D.K.; Pouton, C.W.; Porter, C.J.H. Polymeric Precipitation Inhibitors Promote Fenofibrate Supersaturation and Enhance Drug Absorption from a Type IV Lipid-Based Formulation. Mol. Pharm. 2018, 15, 2355–2371.
  30. Hens, B.; Brouwers, J.; Corsetti, M.; Augustijns, P. Supersaturation and Precipitation of Posaconazole Upon Entry in the Upper Small Intestine in Humans. J. Pharm. Sci. 2016, 105, 2677–2684.
  31. Rubbens, J.; Brouwers, J.; Tack, J.; Augustijns, P. Gastrointestinal dissolution, supersaturation and precipitation of the weak base indinavir in healthy volunteers. Eur. J. Pharm. Biopharm. 2016, 109, 122–129.
  32. Arunprasad K, Narayanan N, Rajalakshmi G. Preparation and Evaluation of Solid Dispersion of Terbinafine Hydrochloride. Vol. 3, International Journal of Pharmaceutical Sciences Review and Research.
  33. Sharma A, Arora K, Mohapatra H, Sindhu RK, Bulzan M, Cavalu S, et al. Supersaturation-Based Drug Delivery Systems: Strategy for Bioavailability Enhancement of Poorly Water-Soluble Drugs. Molecules. 2022;27(9).
  34. Xua S, Dai WG. Drug precipitation inhibitors in supersaturable formulations. Vol. 453, International Journal of Pharmaceutics. Elsevier B.V.; 2013. p. 36–43.
  35. Kumari B, Bishnoi H. Review Article Solid Dispersion?: Its Types And Mechanism Of enhancement of Solubility by Solid Dispersion. Journal of Pharma Research. J Pharma Res. 2019;8(3):65–71.
  36. Saffoon N, Uddin R, Huda NH, Sutradhar KB. Enhancement of oral bioavailability and solid dispersion: A review. J Appl Pharm Sci. 2011;1(7):13–20.
  37. Sridhar I, Doshi A, Joshi B, Wankhede V, Doshi J. Solid Dispersions: an Approach to Enhance Solubility of poorly Water-Soluble Drug. J Sci Innov Res [Internet]. 2013;2(3):685–94.
  38. Mukesh S, Joshi P, Bansal AK, Kashyap MC, Mandal SK, Sathe V, et al. Amorphous Salts Solid Dispersions of Celecoxib: Enhanced Biopharmaceutical Performance and Physical Stability. Mol Pharm. 2021 Jun 7;18(6):2334–48.
  39. Yamashita, K., Nakate, T., Okimoto, K., Ohike, A., Tokunaga, Y., Ibuki, R., Higaki, K.,Kimura, T., 2003. Establishment of new preparation method for solid dispersion formulation of tacrolimus. Int. J. Pharm. 267, 79–91.
  40. Chen, Z.Q., Liu, Y., Zhao, J.H., Wang, L., Feng, N.P., 2012. Improved oral bioavailability of poorly water-soluble indirubin by a super saturatable self-micro emulsifying drug delivery system. Int. J. Nanomed. 7, 1115–1125.
  41. Tajarobi, F., Larsson, A., Matic, H., Abrahmsén-Alami, S., 2011. The influence of crystallization inhibition of HPMC and HPMCAS on model substance dissolution and release in swellable matrix tablets. Eur. J. Pharm. Biopharm. 78, 125–133.
  42. Zhang, N., Zhang, W., Jin, Y., Quan, D.-Q., 2011. Studies on preparation of carbamazepine (CBZ) supersaturatable self-microemulsifying (S-SMEDDS) formulation and relative bioavailability in beagle dogs. Pharm. Dev. Technol. 16, 415–421.
  43. Tang, B.; Cheng, G.; Gu, J.C.; Xu, C.H. Development of solid self-emulsifying drug delivery systems: Preparation techniques and dosage forms. Drug Discov. Today 2008, 13, 606–612. [CrossRef]
  44. Dokania, S.; Joshi, A.K. Self-microemulsifying drug delivery system (SMEDDS)–challenges and road ahead. Drug Deliv. 2015, 22, 675–690. [CrossRef]
  45. Herpin, M.J.; Smyth, H.D. Super-heated aqueous particle engineering (SHAPE): A novel method for the micronization of poorly water-soluble drugs. J. Pharm. Investig. 2018, 48, 135–142. [CrossRef]
  46. Chavan, R.B.; Modi, S.R.; Bansal, A.K. Role of solid carriers in pharmaceutical performance of solid supersaturable SEDDS of celecoxib. Int. J. Pharm. 2015, 495, 374–384. [CrossRef]
  47. Pinto, J.M.O.; Leão, A.F.; Bazzo, G.C.; Mendes, C.; Madureira, L.M.P.; Caramori, G.F.; Parreira, R.L.T.; Stulzer, H.K. Supersaturating drug delivery systems containing fixed-dose combination of two antihypertensive drugs: Formulation, in vitro evaluation and molecular metadynamics simulations. Eur. J. Pharm. Sci. 2021, 163, 105860. [CrossRef]

Photo
MANOJ R. V.
Corresponding author

Department of Pharmaceutics, Sarada Vilas College of Pharmacy, Mysore.

Photo
Parthasarathi K. Kulkarni
Co-author

Department of Pharmaceutics, Sarada Vilas College of Pharmacy, Mysore.

Photo
Nagendra R.
Co-author

Department of Pharmaceutics, Sarada Vilas College of Pharmacy, Mysore.

Photo
Venkatesh K.
Co-author

Department of Pharmaceutics, Sarada Vilas College of Pharmacy, Mysore.

Photo
Hanumanthachar Joshi
Co-author

Department of Pharmacognosy, Sarada Vilas College of Pharmacy, Mysore.

Manoj R. V., Parthasarathi K. Kulkarni, Nagendra R., Venkatesh K. , Supersaturated Drug Delivery System: An Approach To Enhance The Bioavailability, Int. J. of Pharm. Sci., 2024, Vol 2, Issue 2, 145-153. https://doi.org/10.5281/zenodo.10625380

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