In vitro evaluation of poloxamer in situ forming gels for bedaquiline fumarate salt and pharmacokinetics following intramuscular injection in rats

Hemelryck, Sandy Van; Dewulf, Jonatan; Niekus, Harm; Heerden, Marjolein van; Ingelse, Benno; Holm, René; Mannaert, Erik; Langguth, Peter

doi:10.1016/j.ijpx.2019.100016

Cited by 20 publications

(18 citation statements)

References 19 publications

(38 reference statements)

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“…The dissolution profile of the empty formulation is shown in Figure 9 . As previously confirmed by other authors, the dissolution of the hydrogel occurs constantly and rapidly, that is, virtually 100% after 24 h [ 48 ]. This result is probably due to the high solubility of P407 in aqueous media and this is important for the design of an in situ gelling formulation because the dissolution properties modulate the drug leakage at the administration site [ 83 ].…”

Section: Resultssupporting

confidence: 76%

“…Thanks to their versatility, these formulations could be employed for various biomedical applications and administration routes (e.g., subcutaneous or intramuscular) [45,48,84,86]. For examples, previous studies demonstrated that rutin significantly increases the fibroblast proliferation and the collagen production, being a support in wound-healing therapy [33].…”

Section: Discussionmentioning

confidence: 99%

“…Gel dissolution studies were performed in triplicate and based on the gravimetric method [ 47 , 48 ]. 1 mL of liquid formulation (4 °C) was added to a pre-weighed glass vial and equilibrated at 37 °C for at least 10 min with the aim of promoting gelation.…”

Section: Methodsmentioning

confidence: 99%

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Rutin-Loaded Poloxamer 407-Based Hydrogels for In Situ Administration: Stability Profiles and Rheological Properties

et al. 2020

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Rutin is a flavone glycoside contained in many plants, and exhibits antioxidant, anti-inflammatory, anticancer, and wound-healing properties. The main disadvantage related to the use of this molecule for pharmaceutical application is its poor bioavailability, due to its low solubility in aqueous media. Poloxamer 407-hydrogels show interesting thermo-sensitive properties that make them attractive candidates as pharmaceutical formulations. The hydrophobic domains in the chemical structure of the copolymer, a polymer made up of two or more monomer species, are useful for retaining poorly water-soluble compounds. In this investigation various poloxamer 407-based hydrogels containing rutin were developed and characterized as a function of the drug concentration. In detail, the Turbiscan stability index, the micro- and dynamic rheological profiles and in vitro drug release were investigated and discussed. Rutin (either as a free powder or solubilized in ethanol) did not modify the stability or the rheological properties of these poloxamer 407-based hydrogels. The drug leakage was constant and prolonged for up to 72 h. The formulations described are expected to represent suitable systems for the in situ application of the bioactive as a consequence of their peculiar versatility.

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Section: Resultssupporting

confidence: 76%

Section: Discussionmentioning

confidence: 99%

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Rutin-Loaded Poloxamer 407-Based Hydrogels for In Situ Administration: Stability Profiles and Rheological Properties

et al. 2020

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“…For example, poloxamer 407 gels offer weak mechanical strength for applications under shear [ 60 ] as a result of the shear thinning character, [ 104 ] rapid dissolution, [ 105 ] and weak mucoadhesion. [ 106 ] Consequently, poloxamer 407 gels display poor residence times in vivo, with one study estimating that ≈60% of a poloxamer gel was removed from the vagina of mice after 1 h. [ 107,108 ] Additionally, minor dilution may elevate T gel above body temperature and reverse gelation, as seen in vivo after ocular administration. [ 18 ] There is a need for novel thermoreversible gelators, but crucially these materials must offer clear advantages over poloxamer 407 where the expense of translating technologies is substantial and risk of failure must be mitigated during material development.…”

Section: Thermoreversible Gelatorsmentioning

confidence: 99%

Polymers Exhibiting Lower Critical Solution Temperatures as a Route to Thermoreversible Gelators for Healthcare

Cook

Haddow

Kirton

et al. 2020

Adv Funct Materials

129

113

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The ability to trigger changes to material properties with external stimuli, so‐called “smart” behavior, has enabled novel technologies for a wide range of healthcare applications. Response to small changes in temperature is particularly attractive, where material transformations may be triggered by contact with the human body. Thermoreversible gelators are materials where warming triggers reversible phase change from low viscosity polymer solution to a gel state. These systems can be generated by the exploitation of macromolecules with lower critical solution temperatures included in their architectures. The resultant materials are attractive for topical and mucosal drug delivery, as well as for injectables. In addition, the materials are attractive for tissue engineering and 3D printing. The fundamental science underpinning these systems is described, along with progress in each class of material and their applications. Significant opportunities exist in the fundamental understanding of how polymer chemistry and nanoscience describe the performance of these systems and guide the rational design of novel systems. Furthermore, barriers to translating technologies must be addressed, for example, rigorous toxicological evaluation is rarely conducted. As such, applications remain tied to narrow fields, and advancements will be made where the existing knowledge in these areas may be applied to novel problems of science.

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“…From the results of the study obtained results that there was an increase of each polymer, stable does not show any meaningful changes, and there is a continuous release of the drug for 6 hours, to treat periodontal. In situ formulations of poloxamer gel 388 and poloxamer 407 for intramuscular injection use showed results that poloxamer in situ formed the gel for about 6 hours as well as having a continuous release of the drug in the short term observed in mice for up to 24 hours (Hemelryck et al, 2019).…”

Section: Poloxamer (Pm) Combination Gel Forming Agent Formulationmentioning

confidence: 99%

The Advantages of In situ Gel from Every Different Formulation

Sopyan¹,

Intani²,

S³

et al. 2020

ijrps

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The in situ gel system is one of the polymer-based solutions that show the sol phase transition to gel. In addition to being used to improve bioavailability, this gel is also used to make the drug increase the residence time in the area of use, so that it can provide maximum effectiveness via enhancing of per cent permeation, The use of in situ gel, usually used in ocular administration of drugs, for the treatment of cancer, administration of drugs in the vaginal, rectal, topical, oral, and any route administration. There are many formulations of in situ gel formation that are used for medicinal preparations for many purposes, with different lengths of stay. Searching for articles is done online, browsing the PubMed and Google scholar site with the keyword "Formulation In situ Gel". The fourty articles used, there were 40 in situ gel formulations with gelling agents and also different uses. The purpose of this article review is to look at the superiority of in situ gel formulations and to compare various in situ gel formulations studied from 40 articles used, so that it can be seen which formulation is most often used and has a good effect on drugs preparations.

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In vitro evaluation of poloxamer in situ forming gels for bedaquiline fumarate salt and pharmacokinetics following intramuscular injection in rats

Abstract: Graphical abstract

Cited by 20 publications

References 19 publications

Rutin-Loaded Poloxamer 407-Based Hydrogels for In Situ Administration: Stability Profiles and Rheological Properties

Rutin-Loaded Poloxamer 407-Based Hydrogels for In Situ Administration: Stability Profiles and Rheological Properties

Polymers Exhibiting Lower Critical Solution Temperatures as a Route to Thermoreversible Gelators for Healthcare

The Advantages of In situ Gel from Every Different Formulation

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