Recent and Relevant Methodology in the Advancement of Solid Dispersion
Most of the promising drugs in development channels are poorly water-soluble drugs which limit formulation approaches, clinical application because of their low dissolution and bioavailability. And the major current challenges of the pharmaceutical industry are apropos strategies that improve the water solubility of drugs.
Solid dispersion has been considered one of the major evolutions in overcoming these issues with several successfully marketed products. Though solid dispersion has been outlined as an efficient drug delivery system, the design of specific dosage forms for pharmaceutical therapy is necessary to improve the solubility and bioavailability of poorly water-soluble drugs.
Solid dispersion can be prepared by several methods such as solvent evaporation, melting, and supercritical fluid technology. This review intends to provide an updated overview of the recent trends over the past few years in solid dispersion preparation techniques and polymer used. Along with the various pharmaceutical strategies and future visions for the solubilization of poorly water-soluble drugs
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Table 1: Summary related to overall techniques used recently with continually used polymer
| SD Techniques | Drugs | Polymers | Ref. |
|---|---|---|---|
| Solvent evaporation | Dutasteride (DUT) | Microcrystalline cellulose | [16] |
| Oleanolic acid (OA) | Leucine | [17] | |
| Efonidipine hydrochloride | HPMC-AS | [18] | |
| Sirolimus | Polyvinylpyrrolidone (PVP), Poloxamer 188 and Cremophore RH40 | [19] | |
| Febuxostat (FB) | Polyvinylpyrrolidone (PVP K30) and poloxamer | [20] | |
| Ticagrelor | TPGS and Neusilin® US2 | [21] | |
| Candesartan cilexetil (CC) | Tromethamine (Tris) | [22] | |
| Progesterone (PG) | Hydroxypropyl methylcellulose (HPMC), Hydroxypropyl methylcellulose acetate succinate (HPMCAS), Microcrystalline cellulose (MCC), Polyvinylpyrrolidone (PVP) and silica (SiO2) | [23] | |
| Andrographolide (ADG) | Silica (SiO2) | [24] | |
| Hot melt extrusion | Fenofibrate (FNB) | PVP VA64 | [28] |
| Baicalein | Kollidon VA64 and Eudragit EPO | [29] | |
| Indomethacin (IND), Itraconazole (ITZ), and Griseofulvin (GSF) | Eudragit EPO, Eudragit L-100-55, Eudragit L-100, HPMCAS-LF, HPMCAS-MF, Pharmacoat 603, and Kollidon VA-64 | [30] | |
| Indomethacin (IND) | Magnesium aluminium and lithium magnesium sodium silicates | [31] | |
| Carbamazepine (CBZ) | Eudragit EPO | [33] | |
| Osthole (OS) | Plasdone S-630, HPMC-E5, Eudragit EPO, and Soluplus | [34] | |
| Lacidipine | Soluplus and PVP VA64 | [35] | |
| Triamterene | D-mannitol | [36] | |
| Melt agglomeration | Diazepam | Polyethylene glycol (PEG) 3000 or Gelucire 50/13 | [39] |
| Lu-X | Rylo MG12, Gelucire 50/13, PEG 3000, or poloxamer 188 | [41] | |
| Lumefantrine | Polyethylene glycol (PEG) 6000 or Poloxamer 188 | [42] | |
| Spray drying method | Indomethacin (IMC) | Polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol | [44] |
| Ibuprofen | Curcumin | [45] | |
| Candesartan cilexetil (CC) | PVPK30 | [46] | |
| Pioglitazone | PVP K17, PVP K30, and HPMC E3 | [47] | |
| Darunavir | Hydroxypropyl methylcellulose (HPMC), hydroxypropyl methylcellulose acetate succinate (HPMC AS) and polyvinylpyrrolidone K-30 (PVP) | [48] | |
| Tadalafil (TDL) | Glycyrrhizin | [49] | |
| Nisoldipine | Polyethylene glycol 4000 (PEG4000) | [50] | |
| Ketoprofen | vinyl-pyrrolidone based polymers | [51] | |
| Efavirenz | Polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer (Soluplus®) | [52] | |
| Lyophilization | Efavirenz | Polyvinylpyrrolidone (PVP) K-30 | [55] |
| Famotidine | Soluplus® (SP) | [56] | |
| Prednisolone | Bovine serum albumin (BSA) | [57] | |
| Diclofenac sodium (DS) | Ethylcellulose (ECand chitosan (CS)) | [58] | |
| Mebendazole (MBZ) | low-substituted hydroxypropylcellulose (L-HPC) | [59] | |
| Exemestane | Phospholipid/sodium deoxycholate | [60] | |
| Valsartan (VAL) | Polyethylene glycol 6000 (PEG6000) and hydroxypropylmethylcellulose | [61] | |
| Telmisartan | Polyvinylpyrrolidone (PVP) K30 | [62] | |
| Tadalafil (Td) | HPMC, MC, PVP, PVP-VA, Kollicoat IR and Soluplus | [63] | |
| Fusion method | Torcetrapib, itraconazole, and lopinavir | HPMCAS (L, M, and H), copovidone, Soluplus, PEG1500, Vitamin-E TPGS, Kolliphor EL, and Eudragit | [64] |
| Spironolactone (SPL) | Polyethylene glycol 4000 (PEG 4000) | [65] | |
| Itraconazole | Eudragit E100 | [66] | |
| Efavirenz | Polyethylene glycol8000, polyvinylpyrrolidone K30 | [67] | |
| Thiocolchicoside (TCS) | Poloxamer-188 | [69] | |
| Piroxicam | Solutol and Gelucire | [70] | |
| Atorvastatin calcium, cefuroxime axetil, clotrimazole, ketoconazole and metronidazole benzoate | Citric acid and sodium bicarbonate | [71] | |
| Atorvastatin | Polyvinyl pyrrolidone K30 (PVP), polyethylene glycol 6000 (PEG), Soluplus®, and chitosan | [73] | |
| Carvedilol (CARV) | Polyvinylpyrrolidone (PVP), hydroxypropyl methylcellulose (HPMC), Soluplus® and Eudragit® | [74] | |
| Cefuroxime axetil (CA) | Silica | [77] | |
| Glyburide | Silica | [78] | |
| Bifendate | Poly (ethylene oxide) (PEO) | [79] | |
| Budesonide | Polyethylene glycol 4000 and 6000 and | [80] | |
| Cefixime trihydrate | Soluplus | [81] | |
| Furosemide | Crospovidone | [82] | |
| Co- precipitation method | Quercetin (Que) | HPMCAS-HF, HPMCAS-MF and HPMCAS-LF | [83] |
| Lumefantrine | HydroxypropylmethylcellulosePhthalate (HPMCP), hydroxypropylmethylcellulose acetate succinate (HPMCAS), poly (methacrylic acid-ethyl acrylate) (EL100) and cellulose acetate phthalate (CAP) | [86] | |
| Silymarin | HPMC E 15LV | [87] | |
| GDC-0810 | Hydroxypropyl methylcellulose acetate succinate | [88] | |
| Electrospinning | Ibuprofen (IBU) | HPMCAS and HPMCP-HP55 | [92] |
| Itraconazole (ITRA) | PVPVA64 | [93] | |
| Spironolactone | Poly (vinylpyrrolidone-co-vinyl acetate) | [94] | |
| Itraconazole [ITR] | Polyvinylpyrrolidone-vinyl acetate | [95] | |
| Meloxicam | Eudragit E | [98] |
Article information: Talla S, Wadher K, Umekar M, Lohiya R. Recent and Relevant Methodology in the Advancement of Solid Dispersion. JDDT [Internet]. 15Aug.2021 [cited 20Aug.2021];11(4-S):247-5. Available from: http://jddtonline.info/index.php/jddt/article/view/4963
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