Hypromellose – A traditional pharmaceutical excipient with modern applications in oral and oromucosal drug delivery

Mašková, Eliška; Kubová, Kateřina; Raimi-Abraham, Bahijja Tolulope; Vllasaliu, Driton; Vohlídalová, Eva; Tuřánek, Jaroslav; Mašek, Josef

doi:10.1016/j.jconrel.2020.05.045

Cited by 143 publications

(68 citation statements)

References 289 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…Therefore, a plasticizer was added (5% m/m) to reduce the extrusion temperature to 100 °C. TEC was selected for being a versatile plasticizer agent for several HME polymers [ 34 ].…”

Section: Resultsmentioning

confidence: 99%

“…Although the thermal decomposition of this salt occurs at 120 • C [33], the extrusion shear anticipated this event to lower temperatures. Therefore, a plasticizer was added (5% m/m) to reduce the extrusion temperature to 100 • C. TEC was selected for being a versatile plasticizer agent for several HME polymers [34].…”

Section: Initial Trials and Extrusion Setupmentioning

confidence: 99%

See 1 more Smart Citation

Hot-Melt Extrusion as an Advantageous Technology to Obtain Effervescent Drug Products

et al. 2020

View full text Add to dashboard Cite

Here, we assessed the feasibility of hot-melt extrusion (HME) to obtain effervescent drug products for the first time. For this, a combined mixture design was employed using paracetamol as a model drug. Extrudates were obtained under reduced torque (up to 0.3 Nm) at 100 °C to preserve the stability of the effervescent salts. Formulations showed vigorous and rapid effervescent disintegration (<3 min), adequate flow characteristics, and complete solubilization of paracetamol instantly after the effervescent reaction. Formulations containing PVPVA in the concentration range of 15–20% m/m were demonstrated to be sensitive to accelerated aging conditions, undergoing marked microstructural changes, since the capture of water led to the agglomeration and loss of their functional characteristics. HPMC matrices, in contrast, proved to be resistant to storage conditions in high relative humidity, showing superior performance to controls, including the commercial product. Moreover, the combined mixture design allowed us to identify significant interactions between the polymeric materials and the disintegrating agents, showing the formulation regions in which the responses are kept within the required levels. In conclusion, this study demonstrates that HME can bring important benefits to the elaboration of effervescent drug products, simplifying the production process and obtaining formulations with improved characteristics, such as faster disintegration, higher drug solubilization, and better stability.

show abstract

“…Therefore, a plasticizer was added (5% m/m) to reduce the extrusion temperature to 100 °C. TEC was selected for being a versatile plasticizer agent for several HME polymers [ 34 ].…”

Section: Resultsmentioning

confidence: 99%

Section: Initial Trials and Extrusion Setupmentioning

confidence: 99%

Hot-Melt Extrusion as an Advantageous Technology to Obtain Effervescent Drug Products

et al. 2020

View full text Add to dashboard Cite

show abstract

“…Processing ASD into nanoparticles as means of formulation has also been frequently considered as a desirable strategy for increasing the therapeutical windows of highly potent compounds [61,[146][147][148][149][150]. Examples of amorphous drug-polymer nanoparticle formulations exhibiting enhanced in vitro and in vivo performances are summarized in Table 3.…”

Section: The Importance Of Polymeric Excipients For Drug Permeability Enhancementmentioning

confidence: 99%

“…On the other hand, the mucoadhesive drug delivery system (MDDS) featuring a longer adhesion time and subsequent penetration through the epithelial membrane is also a desirable formulation design. Polymers such as HPMC, thiolated polymers, polysaccharides, or maleimide modified polymers were reported for the MDDS [61,150,[155][156][157]. The raloxifene loaded suspension nanoparticles were found to be 3.3-fold and 2.3-fold higher, in terms of AUC and C max increment, respectively, in plasma than those of the drug powder.…”

Section: The Importance Of Polymeric Excipients For Drug Permeability Enhancementmentioning

confidence: 99%

“…In this review, we highlight: (i) the thermodynamics and kinetics associated with the formation of drug-rich phases from the dissolution (Section 2); (ii) in vitro permeability enhancement and in vivo bioavailability enhancement in the context of ASD formulation (Section 3). Other aspects associated with the drug-rich phases, such as the dissolution model [58], the liquid-liquid phase separation (LLPS) identification and screening technique [59], and the impact of surfactants and polymers in the nanodroplet uptake [60,61], can be found in other excellent studies in the literature.…”

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Drug-Rich Phases Induced by Amorphous Solid Dispersion: Arbitrary or Intentional Goal in Oral Drug Delivery?

et al. 2021

View full text Add to dashboard Cite

Among many methods to mitigate the solubility limitations of drug compounds, amorphous solid dispersion (ASD) is considered to be one of the most promising strategies to enhance the dissolution and bioavailability of poorly water-soluble drugs. The enhancement of ASD in the oral absorption of drugs has been mainly attributed to the high apparent drug solubility during the dissolution. In the last decade, with the implementations of new knowledge and advanced analytical techniques, a drug-rich transient metastable phase was frequently highlighted within the supersaturation stage of the ASD dissolution. The extended drug absorption and bioavailability enhancement may be attributed to the metastability of such drug-rich phases. In this paper, we have reviewed (i) the possible theory behind the formation and stabilization of such metastable drug-rich phases, with a focus on non-classical nucleation; (ii) the additional benefits of the ASD-induced drug-rich phases for bioavailability enhancements. It is envisaged that a greater understanding of the non-classical nucleation theory and its application on the ASD design might accelerate the drug product development process in the future.

show abstract

Biopolymers for Vaginal Delivery

Kanojiya,

Karemore,

Wadetwar

2024

Biopolymers in Pharmaceutical and Food Applications

View full text Add to dashboard Cite

Hypromellose – A traditional pharmaceutical excipient with modern applications in oral and oromucosal drug delivery

Cited by 143 publications

References 289 publications

Hot-Melt Extrusion as an Advantageous Technology to Obtain Effervescent Drug Products

Hot-Melt Extrusion as an Advantageous Technology to Obtain Effervescent Drug Products

Drug-Rich Phases Induced by Amorphous Solid Dispersion: Arbitrary or Intentional Goal in Oral Drug Delivery?

Biopolymers for Vaginal Delivery

Contact Info

Product

Resources

About