Effect of poloxamer on physicochemical properties of tacrolimus solid dispersion improving water solubility and dissolution rate

Ha, Jung-Myung; Kang, Seung-Yeob; Park, Chun‐Woong; Bin, Sung-A; Rhee, Yun-Seok; Seo, Jeong-Woong; Kim, Su-Heon; Chi, Sang-Cheol; Park, Eun-Seok

doi:10.1007/s40005-012-0025-4

Cited by 17 publications

(7 citation statements)

References 27 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Moreover, drug-polymer [8] ). Maniruzzaman et al [8] Felodipine-Eudragit E PO, Eudragit NE 30D Raman, FTIR, NMR Nollenberger et al [112] Griseofulvin-polymers, indomethacin-polymers, itraconazole-polymers Polymers: Eudragit E PO, Eudragit L100-55, Eudragit L100, HPMC AS-LF, HPMC AS-MF, Pharmacoat 603, PVP VA FTIR Sarode et al [110] Hydrochlorothiazide-Hybrane S1200 FTIR Ravina-Eirin et al [5] Ibuprofen-ethylcellulose FTIR De Brabander et al [48] Indomethacin-Eudragit E PO FTIR Qi et al [21] and Liu et al [134] Itraconazole-Carbopol 974P DSC Miller et al [120] Ketoprofen-PEO Raman Schachter et al [146] Mefenamic acid-Poloxamer 188 DSC, Raman Andrews et al [131] Methylparaben-Eudragit RS PO NMR Wu and McGinity [44] Metoprolol tartrate-Kollidon SR DSC, FTIR, Raman Saerens et al [135] Metoprolol tartrate-Eudragit RS PO Raman Saerens et al [136] Naproxen-Eudragit E PO FTIR Kindermann et al [11] Nifedipine-ethylcellulose DSC, FTIR Huang et al [17] Nimodipine-Eudragit E PO, HPMC, PVP VA FTIR Zheng et al [49] Tacrolimus-Poloxamer FTIR Ha et al [98] DSC, differential scanning calorimetry; FTIR, Fourier transform infrared spectroscopy; HPMC AS, hydroxypropyl methylcellulose acetate succinate; NMR, nuclear magnetic resonance; PVP, poly(vinyl pyrrolidinone); PVP PA, poly(vinyl pyrrolidone-co-vinyl acetate); XPS, X-ray photoelectron spectroscopy.…”

Section: Discussionmentioning

confidence: 99%

“…Disruption of the crystal lattice and lack of long‐range order render the amorphous drug in a high‐energy state. Thus, amorphous drug is associated with higher solubility to form supersaturated solution . Secondly, the high shear force introduced during the extrusion process may disperse drug and polymer at molecular level to increase the possibility of drug–polymer interactions, which favour the dissolution of drug …”

Section: Effects Of Drug–polymer Interactions On Drug Dissolving Processmentioning

confidence: 99%

See 1 more Smart Citation

Interactions between drugs and polymers influencing hot melt extrusion

Pang

Guo

et al. 2014

Journal of Pharmacy and Pharmacology

118

View full text Add to dashboard Cite

Objectives Hot melt extrusion (HME) as a technique for producing amorphous solid dispersion (ASD) has been widely used in pharmaceutical research. The biggest challenge for the application of HME is the thermal degradation of drug, poor physical stability of ASD and precipitation of drug during dissolution. Interactions between drugs and polymers may play an important role in overcoming these barriers. In this review, influence of drug-polymer interactions on HME and the methods for characterizing the drug-polymer interactions were reviewed. Key findings Strong drug-polymer interactions, especially ionic interactions and hydrogen bonds, are helpful to improving the thermal stability of drug during HME, enhancing the physical stability of ASD during storage and maintaining supersaturated solution after dissolution in gastrointestinal tract. The interactions can be quantitatively and qualitatively characterized by many analysing methods. Conclusions As many factors collectively determine the properties of HME products, drug-polymer interactions play an extremely important role. However, the action mechanisms of drug-polymer interactions need intensive investigation to provide more useful information for optimizing the formulation and the process parameters of HME.

show abstract

Section: Discussionmentioning

confidence: 99%

Section: Effects Of Drug–polymer Interactions On Drug Dissolving Processmentioning

confidence: 99%

Interactions between drugs and polymers influencing hot melt extrusion

Pang

Guo

et al. 2014

Journal of Pharmacy and Pharmacology

118

View full text Add to dashboard Cite

show abstract

“…The dissolution of tacrolimus was also reported to be increased using the solid dispersion method with poloxamers 188 and 407. This result was due to the conversion of tacrolimus to the amorphous phase, leading to increased solubility (Ha et al, 2012). Another study confirmed the better characteristics of poloxamer 188 than poloxamer 407 in improving dissolution; this performance was related to the higher proportion of oxyethylene segments in poloxamer 407, which retarded dissolution (Medarević et al, 2016).…”

Section: Solubilitymentioning

confidence: 90%

Mini-Review of Poloxamer as a Biocompatible Polymer for Advanced Drug Delivery

Nugraha

Anggadiredja

Rachmawati

2022

Braz. J. Pharm. Sci.

View full text Add to dashboard Cite

Poloxamer is a biocompatible polymer that has already been approved by the US FDA for multiple applications. Poloxamer itself has many grades and functional categories that enable the improvement of both physicochemical and biological properties of drugs. In this minireview, the functional properties of poloxamer for physicochemical modification, such as solubility and stability, and biological response modification, such as neuroprotection, cell apoptosis, efflux pump modification, membrane cell modification, and cellular uptake, are discussed to provide a broader understanding to assist the development of poloxamer-based formulations.

show abstract

“…Tacrolimus as a macrolide has immunomodulatory effects and is about 10-100 times more potent than cyclosporine A in the same mechanism of action; 1 however poor aqueous solubility is the main limiting factor for its application. 22 Systemic uses of Tacrolimus in treatment of ophthalmic immune-mediated problems such as uveitis, eyes dryness following graft-versus-host disease, corneal transplants and ocular pemphigoid is routine. 1 In case of topical eye drop formulations; Tacrolimus 0.03% in olive oil was introduced and showed to be effective in improving the symptoms of severe allergic conjunctivitis.…”

Section: Discussionmentioning

confidence: 99%

Preliminary In Vivo Safety Evaluation of a Tacrolimus Eye Drop Formulation Using Hydroxypropyl Beta Cyclodextrin After Ocular Administration in NZW Rabbits

Mahmoudi¹,

Malaekeh‐Nikouei²,

Hanafi‐Bojd³

et al. 2020

OPTH

View full text Add to dashboard Cite

Aim: Tacrolimus is an immunosuppressive drug with higher potency compared to cyclosporine A (as a useful immunosuppressant). We prepared an ophthalmic solution formulation of Tacrolimus using hydroxypropyl beta cyclodextrin (HP-ßCD). In the present study, safety of this formulation was investigated in rabbits. Materials and Methods: Formulation containing HP-ßCD, Tacrolimus, Polyvinyl alcohol (PVA) and Benzalkonium Chloride in PBS 7.4 was prepared. Tacrolimus concentration in ophthalmic preparation was 0.05% w/v. Ten male New Zealand white rabbits were housed in clean separated cages. One drop of Tacrolimus prepared formulation and a placebo formulation were applied every 12 hrs in the right and left eyes respectively, for 28 days. Results: This new aqueous formulation of Tacrolimus could improve Tacrolimus solubility about 42 times. Clinical examinations on the 1st, 3rd, 7th, 14th and 28th days of study showed transient redness and conjunctivitis in some cases of both control and intervention groups that was not persistent. At the end of the study, there were no statistical differences between the two groups in corneal epithelial defect, redness or pathological evaluations. Conclusion: The results of this study suggest that eye drop formulation of CD-Tacrolimus is safe in preliminary evaluations and can be useful for further studies.

show abstract

Effect of poloxamer on physicochemical properties of tacrolimus solid dispersion improving water solubility and dissolution rate

Cited by 17 publications

References 27 publications

Interactions between drugs and polymers influencing hot melt extrusion

Interactions between drugs and polymers influencing hot melt extrusion

Mini-Review of Poloxamer as a Biocompatible Polymer for Advanced Drug Delivery

<p>Preliminary I<em>n</em> V<em>ivo</em> Safety Evaluation of a Tacrolimus Eye Drop Formulation Using Hydroxypropyl Beta Cyclodextrin After Ocular Administration in NZW Rabbits</p>

Contact Info

Product

Resources

About