Supersaturation-Based Drug Delivery Systems: Strategy for Bioavailability Enhancement of Poorly Water-Soluble Drugs
Abstract
:1. Introduction
2. Supersaturated Drug Delivery Systems
2.1. Precipitation Inhibitors
S.NO | Formulation (Spring Form) | Precipitation Inhibitors (Parachute) | Model Drug | In-Vivo and In-Vitro Performance (PK) | Reference |
---|---|---|---|---|---|
1. | Solid dispersion | PEG 6000, PVP, HPMC | Tacrolimus | HPMC When compared to crystalline powder administration, there was a 10 fold increase in Cmax and AUC. | [14] |
2. | self-emulsifying drug delivery systems (SEDDS) | PEG 6000, PVP, HPMC | Paciltaxel | HPMC resulted in a 20-fold increase in Cmax and 10-fold increase in oral bioavailability | [15] |
3. | solid dispersions | HPMC, HPMCAS L, M, H SOL | Candesartan Cilexetil | HPMCAS M presented good anti-precipitation efficacy in both media, reaching higher AUC maintainind drug supersaturation for up to 120 min | [16] |
4. | Soild Dispersion | SOL, SLS, P188, PS20 | Chlorthalidone | SOL-SLS complex impacted positively release and Physical stability of chlorthalidone | [17] |
5. | Solid dispersion | SA, SLS | All SDs, demonstrated no drug recrystallization after 34 months of storage exception being those prepared with SA alone or SA-SLS at high drug loading | [18] | |
6. | Solid dispersion | P188, F127, SDS, HS15, ST and TPGS | Lacidipine | Nearly 3.3 and 3.7-fold increase in Cmax and AUC (0–∞) respectively was attained with formulation based on LCDP/SOL/SDS | [19] |
7. | Amorphous Solid dispersion | Eudragit EPO | Trimethoprin and sulfhmethooxazole | The 70% polymer formulation was able to produce and sustain the supersaturated phase of both compounds for 24 h. When compared to the combination of agents, improved antimicrobial effect was observed. | [20] |
8. | Amorphous Solid dispersion | hydroxypropylmethylcellulose acetate succinate (HPMCAS) type M | Candesartan cilexetil | Reduced the desupersaturation of both drugs | [21] |
9. | Amorphous Solid dispersion | Saccharin (SAC) | Griseofulvin | AUC increased 20% in comparison to conventional formulation | [22] |
10. | Soild dispersion | HPMC | Magnolol | Increased the bioavailability (the relative bioavailability was 213.69% | [23] |
11. | SEDDS | PEG 400, Tween 80, Miglyol 812 N | Carbamazepin | When compared to the commercial formulation, 200 mg of dosage resulted in 6.7 and 5.9 times larger increases in Cmax AUC, respectively. | [24] |
12. | SEDDS | HPMC-E5 PVP-12PF | Celecoxib | When comparison to solution and conventional capsule formulations, excellent IVIVC and Human PK was observed. | [25] |
13. | SEDDS | Soluplus | In comparison to drug powder, there was a 2.34-fold increase in Cmax and a 4.82-fold rise in AUC. | [26] | |
14. | SEDDS | Soluplus, PVP VA64, poloxamer 407, PEG 6000 | Celecoxib | PI effect of Soluplus is greater than PEG 6000 PVP, VA64, poloxamer 407 & PEG 6000 | [27] |
15. | SEDDS | Eudragit E PO | Curcumin | A 50 mg/kg dose of PI resulted in a 1.22 and 53.14-fold enhancement in absorption in rabbits when compared to the aqueous phase and standard SEDDS without PI, respectively. | [28] |
16. | SEDDS | Polyvinylpyrrolidone (PVP), hydroxypropyl methyl cellulose (HPMC) | Curcumin | The increased concentration-dependent effect was observed for PVP-K30 when used as PI in comparison to PVP-K90 without PI &HPMC. | [29] |
17. | SEDDS | HPMC K100 | Docetaxel | When SD rats were given a dose of 10 mg/kg, their AUC jumped by around 8.77 times which was 1.45-fold higher than the increases seen with the powder medication and traditional SEDDS without PI. | [30] |
18. | SEDDS | HPMC (5%, w/w) | Ginger extract | SD rats were given a dosage of 100 mg/kg in experimental model of animals, 6-gingerol and 8-gingerol had three time the antioxidant activity (BA) of the unformulated extract, i.e., control rats. | [31] |
19. | SEDDS | HPMC-E5 (5%, w/w) | Glipizide | AUC (2.7-fold) and Cmax (3.4-fold) were found to be increased in Himalayan rabbits when solid su-SEDDS were administered at a dose of 1 mg/kg as compared to the standard drug. | [32] |
20. | SEDDS | Poloxamer, HPMC | Griseofulvin | Aqueous suspension showed three-fold less permeability through the intestinal tract of Wister rats when given a dose of 1 mL at a concentration of 0.05 mg/mL (0.05 mg/mL). | [33] |
21. | SEEDS | HPMC, PEG 4000, PVP-K17 | Indirubin | When compared to the SEDDS without PI, the chemical exhibited better oral absorption and relative BA [129.5%] when delivered in vivo to SD rats at such a dose frequency of 2.58 mg/kg. | [34] |
22. | SEDDS | HPMC-E5LV | Paclitaxel | Compared to the Taxol® formulation and the standard SEDDS, the SD rats administered optimised formulation. At a dosage of 10 mg/kg, the Cmax and AUC were ten-fold and twenty-fold higher, respectively. | [35] |
23. | SEDDS | HPMC-E15LV | Resveratrol | After 20 mg/kg administration to Wistar rats, the su-SEDDS demonstrated a 1.33-fold increase in AUC compared to standard SEDDS lacking PI. | [36] |
24. | SEDDS | HPMC-E50LV | Silybin | SD rats were given a dosage of 533 mg/kg, which resulted in a 3-fold increase in AUC compared to the usual SEDDS without HPMC in vivo. | [37] |
25. | SEDDS | Poloxamer 407, Poloxamer 407 > HPCD, Eudragit L100 HPMCP | Silymarin | Using a dosage of 28 mg/kg of silybinvsLegalon® (a commercialized product) and a 76% BA of su-SEDDS concentration, silybin was evaluated in vivo in rabbits. | [38] |
26. | SEDDS | Soluplus, HPMC, PVP | Tacrolimus | As with conventional SEDDS, the Area under curve and Cmax of su-SEDDS at 1 dose of 5 mg/kg in SD rats were equivalent or larger than conventional SEDDS at the same dosage. | [39] |
27. | SEDDS | Poloxamer 407 | Valsartan | Using a dosage of 10 mg/kg, the medication was put to the test in SD rats. AUC ranges between about 177 and 198%when compared to API and Diovan®, a commercial product. | [40] |
28. | SNEEDS | HPMC, PVP, PVP/VA, and Soluplus® | Aprepitant | Increased dissolution rate of the drug due to enhanced solubility | [41] |
29. | SEDDS | HPMC E5 | Quercetin | improved AUC and Cmax values in comparison to conventional SEDDS | [42] |
30. | SNEDDS | HPMC | Albendazolum | Enhancement in the solubility and oral bioavailability | [43] |
31. | SNEDS | Poloxamer 407 (P 407), Eudragit® L100-55 (Eu), Kolliphor® HS15 (KHS15), Kolliphor® RH40 (K RH40), vitamin E TPGS (vit E TPGS) & Soluplus® | Cinnarizin | 2.7-fold increase in AUC 0–24 h | [44] |
32. | SEDDS | Cremophor RH40 & Macrogol 200 | Cepharanthine | Relative bioavailability was 203.46% | [45] |
33. | SNEDS | Polyoxyethylene (80) sorbitan monooleate (Tween® 80), d-α-tocopherol polyethylene glycol 1000 succinate (d-TPGS, Tocophersolan) | Celecoxib & fenofibrate | SNEDDS development in a short time with manageable resources | [46] |
34. | SMEDDS | PVP | Biphenyl dimethyl dicarboxylate | Significantly increased the Cmax and AUC | [47] |
35. | HPM C, HPMCA, SPV Pluronic F108, | Venetoclax | In vivo exposure of venetoclax was achieved | [48] |
Precipitation Inhibitors’ Influence on Supersaturation
2.2. Supersaturated Drug Delivery Systems (SDDSs) (Spring Form)
2.2.1. Solid Dispersion-Based Supersaturated Drug Delivery Systems (SDDSs)
2.2.2. Supersaturable Lipid-Based Formulations
2.2.3. Transdermal Drug Delivery Systems (TDDSs)
3. Solid Dispersion-Based Supersaturated Drug Delivery Systems (SDDSs) vs. Supersaturable Lipid-Based Formulations
4. Conclusions
Author Contributions
Funding
Data Availability Statement
Acknowledgments
Conflicts of Interest
References
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Sharma, A.; Arora, K.; Mohapatra, H.; Sindhu, R.K.; Bulzan, M.; Cavalu, S.; Paneshar, G.; Elansary, H.O.; El-Sabrout, A.M.; Mahmoud, E.A.; et al. Supersaturation-Based Drug Delivery Systems: Strategy for Bioavailability Enhancement of Poorly Water-Soluble Drugs. Molecules 2022, 27, 2969. https://doi.org/10.3390/molecules27092969
Sharma A, Arora K, Mohapatra H, Sindhu RK, Bulzan M, Cavalu S, Paneshar G, Elansary HO, El-Sabrout AM, Mahmoud EA, et al. Supersaturation-Based Drug Delivery Systems: Strategy for Bioavailability Enhancement of Poorly Water-Soluble Drugs. Molecules. 2022; 27(9):2969. https://doi.org/10.3390/molecules27092969
Chicago/Turabian StyleSharma, Arvind, Kanika Arora, Harapriya Mohapatra, Rakesh K. Sindhu, Madalin Bulzan, Simona Cavalu, Gulsheen Paneshar, Hosam O. Elansary, Ahmed M. El-Sabrout, Eman A. Mahmoud, and et al. 2022. "Supersaturation-Based Drug Delivery Systems: Strategy for Bioavailability Enhancement of Poorly Water-Soluble Drugs" Molecules 27, no. 9: 2969. https://doi.org/10.3390/molecules27092969