Three-dimensional aspects of formulation excipients in drug discovery: a critical assessment on orphan excipients, matrix effects and drug interactions

Veeravalli, Vijayabhaskar; Cheruvu, Hanumanth Srikanth; Srivastava, Pratima; Madgula, Lakshmi Mohan Vamsi

doi:10.1016/j.jpha.2020.02.007

Cited by 14 publications

(7 citation statements)

References 94 publications

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“…However, pluronics are not the only surfactants to exhibit anti-MDR effects ( Livney and Assaraf, 2013 ). Tween® 20, Tween® 80, Myrj® 52, and Brij® 30 inhibit protein kinase C (PKC) activity, modulate Pgp-mediated drug efflux, and decrease the apical efflux of the anthracycline epirubicin across human intestinal epithelial (Caco-2) cells ( Komarov et al, 1996 ; Lo, 2003 ; Tagami et al, 2011 ; Veeravalli et al, 2020 ). Tween 80 has been employed as a surfactant in brain tumor targeting ( Wen et al, 2018 ).…”

Section: Methods Of Preparation For Polymeric Nanoparticles and The Rmentioning

confidence: 99%

Biodegradable Polymeric Nanoparticles for Drug Delivery to Solid Tumors

et al. 2021

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Advances in nanotechnology have favored the development of novel colloidal formulations able to modulate the pharmacological and biopharmaceutical properties of drugs. The peculiar physico-chemical and technological properties of nanomaterial-based therapeutics have allowed for several successful applications in the treatment of cancer. The size, shape, charge and patterning of nanoscale therapeutic molecules are parameters that need to be investigated and modulated in order to promote and optimize cell and tissue interaction. In this review, the use of polymeric nanoparticles as drug delivery systems of anticancer compounds, their physico-chemical properties and their ability to be efficiently localized in specific tumor tissues have been described. The nanoencapsulation of antitumor active compounds in polymeric systems is a promising approach to improve the efficacy of various tumor treatments.

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Section: Methods Of Preparation For Polymeric Nanoparticles and The Rmentioning

confidence: 99%

Biodegradable Polymeric Nanoparticles for Drug Delivery to Solid Tumors

et al. 2021

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“…Medium-chain C8 TJ opening and P-gp inhibitor [44] Cremophor RH40 ® 14-16 Medium-chain C10 TJ opening and P-gp inhibitor [45] Labrafac PG ® 1 Medium-chain.…”

Section: Mixture Of C16 and C18mentioning

confidence: 99%

Liquid and Solid Self-Emulsifying Drug Delivery Systems (SEDDs) as Carriers for the Oral Delivery of Azithromycin: Optimization, In Vitro Characterization and Stability Assessment

et al. 2020

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Azithromycin (AZM) is a macrolide antibiotic used for the treatment of various bacterial infections. The drug is known to have low oral bioavailability (37%) which may be attributed to its relatively high molecular weight, low solubility, dissolution rate, and incomplete intestinal absorption. To overcome these drawbacks, liquid (L) and solid (S) self-emulsifying drug delivery systems (SEDDs) of AZM were developed and optimized. Eight different pseudo-ternary diagrams were constructed based on the drug solubility and the emulsification studies in various SEDDs excipients at different surfactant to co-surfactant (Smix) ratios. Droplet size (DS) < 150 nm, dispersity (Đ) ≤ 0.7, and transmittance (T)% > 85 in three diluents of distilled water (DW), 0.1 mM HCl, and simulated intestinal fluids (SIF) were considered as the selection criteria. The final formulations of L-SEDDs (L-F1(H)), and S-SEDDs (S-F1(H)) were able to meet the selection requirements. Both formulations were proven to be cytocompatible and able to open up the cellular epithelial tight junctions (TJ). The drug dissolution studies showed that after 5 min > 90% and 52.22% of the AZM was released from liquid and solid SEDDs formulations in DW, respectively, compared to 11.27% of the pure AZM, suggesting the developed SEDDs may enhance the oral delivery of the drug. The formulations were stable at refrigerator storage conditions.

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“…Pharmaceutical/formation excipients enhanced the drug potency by inhibiting the drug metabolic pathway or transporter proteins (Veeravalli et al, 2020). Now a day, several surfactants and many natural and synthetic polymeric excipients (Table 2) are used in pharmaceutical formulation as well as in novel drug delivery systems to overcome the effects of P‐gp and deliver the therapeutic agents at the targeted place (Jeganathan et al, 2020; Thomas et al, 2020; Katekar et al, 2020; Mokhtar et al, 2019; Sulheim et al, 2016; Zhang et al, 2017; Liu et al, 2017; Watkins et al, 2017; Valicherla et al, 2016; Hoosain et al, 2015; Constantinides & Wasan, 2007; Veeravalli et al, 2020; Jacob et al, 2020). Berberine (benzylisoquinoline alkaloid) C max , AUC and relative oral bioavailability (404%) enhanced when loaded in Brij‐S20‐modified nanocrystal formulation (Xiong et al, 2018).…”

Section: Approaches To Overcome the Effects Of P‐gpmentioning

confidence: 99%

“…Pharmaceutical/formation excipients play an important role in drug formulation concerning drug delivery at the targeted site and improvement in bioavailability. Pharmaceutical/formation excipients enhanced the drug potency by inhibiting the drug metabolic pathway or transporter proteins (Veeravalli et al, 2020). Now a day, several surfactants and many natural and synthetic polymeric excipients (Table 2) are used in pharmaceutical formulation as well as in novel drug delivery systems to overcome the effects of P‐gp and deliver the therapeutic agents at the targeted place (Jeganathan et al, 2020; Thomas et al, 2020; Katekar et al, 2020; Mokhtar et al, 2019; Sulheim et al, 2016; Zhang et al, 2017; Liu et al, 2017; Watkins et al, 2017; Valicherla et al, 2016; Hoosain et al, 2015; Constantinides & Wasan, 2007; Veeravalli et al, 2020; Jacob et al, 2020).…”

Section: Approaches To Overcome the Effects Of P‐gpmentioning

confidence: 99%

Approaches to minimize the effects of P‐glycoprotein in drug transport: A review

Husain

Makadia

Valicherla

et al. 2022

Drug Development Research

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P-glycoprotein (P-gp) is a transporter protein that is come under the ATP binding cassette family of proteins. It is situated on the surface of the intestine epithelium, where P-gp substrate binds to the transporter and is pumped into the intestine lumen by the ATP-driven energy-dependent process. In this review, we summarize the role of the P-gp efflux transporter situated on the intestine, the clinical importance of P-gp related drug interactions, and approaches to minimize the effect of P-gp in drug transport. This review also focuses on the impact of P-gp on the bioavailability of the orally administered drug. Many drug's oral bioavailabilities can improve by concomitant use of P-gp inhibitors. Multidrug resistance are reduced by using some naturally occurring compounds obtained from plants and several synthetic P-gp inhibitors. Formulation strategies, one of the most important approaches to mimic the P-gp transporter's action, finally enhancing the oral bioavailability of the drug by inhibiting its P-gp efflux. Vitamin E TPGS, Gelucire 44/14 and other pharmaceutical/formulation excipients inhibit the P-gp efflux. A prodrug approach might be a useful strategy to overcome drug resistance.Prodrug helps to enhance the solubility or alter the pharmacokinetic properties but does not diminish the pharmacological action.

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Three-dimensional aspects of formulation excipients in drug discovery: a critical assessment on orphan excipients, matrix effects and drug interactions

Cited by 14 publications

References 94 publications

Biodegradable Polymeric Nanoparticles for Drug Delivery to Solid Tumors

Biodegradable Polymeric Nanoparticles for Drug Delivery to Solid Tumors

Liquid and Solid Self-Emulsifying Drug Delivery Systems (SEDDs) as Carriers for the Oral Delivery of Azithromycin: Optimization, In Vitro Characterization and Stability Assessment

Approaches to minimize the effects of P‐glycoprotein in drug transport: A review

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