Non-ionic Surfactants as a P-Glycoprotein(P-gp) Efflux Inhibitor for Optimal Drug Delivery—A Concise Outlook

Rathod, Sachin; Desai, Heta; Patil, Rahul; Sarolia, Jayant

doi:10.1208/s12249-022-02211-1

Cited by 23 publications

(10 citation statements)

References 111 publications

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“…Tween and Lactoferrin can increase the FEN permeability through the intestinal epithelium. Surfactants also help bioavailability improvement by inhibiting pGP efflux transporter activity …”

Section: Resultsmentioning

confidence: 99%

“…Animals of group I received marketed FEN tablet, group II received FEN-loaded lactoferrin containing SEDDS (FEN Lf-SEDDS), and group III were given FEN suspension in water. Animal dose of FEN (mg/kg body weight) was calculated using the following eq 5: 35 = × AED HED Km (Human correction factor) Km of animal of 250 gm body weight (5) where AED is the animal equivalent dose, and HED is the human equivalent dose.…”

Section: Selection Of Surfactant−cosurfactant By Pseudoternary Phase ...mentioning

confidence: 99%

“…In the last two decades, SEDDS has gained a lot of popularity to deliver highly lipophilic drugs orally. Some of the advatanges of SEDDS include higher stability, lesser chances of phase separation than conventional emulsion, significant improvement of oral bioavailability of lipophilic drug by improving solubility, and possibility of absorption by lymphatic routes. − Some oils and surfactants used in SEDDS are also claimed to be pGP transporter inhibitors, which potentially increases oral bioavailability of pGP substrate drugs . Inside the gastrointestinal tract, mild agitation occurs due to peristalsis, helping SEDDS to form microemulsion or nanoemulsion.…”

Section: Introductionmentioning

confidence: 99%

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Lactoferrin Reduces Surfactant Content in the Self-Emulsifying Drug Delivery System

Khairnar,

Jain,

Chatterjee

2024

ACS Omega

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Self-emulsifying drug delivery systems (SEDDSs) can effectively be employed to formulate drugs with poor oral bioavailability due to low aqueous solubility and high first-pass metabolism. High surfactant content is an existing challenge toward the successful application of SEDDS. A SEDDS is developed with lactoferrin, a natural emulsifier to reduce the Tween content of a fenofibrate (FEN) formulation. FEN SEDDS (SEDDS without lactoferrin) and FEN Lf-SEDDS (SEDDS with lactoferrin) were developed with 30% and 21% Tween content, respectively. Both formulations containing Crodamol GTCC as a lipid component were thermodynamically stable. No significant difference was observed in zeta potential (−9.25 to −12.63 mV), drug content (>85%), and percentage transmittance (>99%) between the two formulations. FEN Lf-SEDDS resulted in higher viscosity and larger particle size than FEN SEDDS. Solidified SEDDS with Aerosil 200 significantly improved in vitro drug release from both formulations than pure FEN. However, FEN SEDDS and FEN Lf-SEDDS did not show a significant difference in cumulative percent release or dissolution efficiency at 120 min. It can be concluded that lactoferrin containing SEDDS with 27% lesser synthetic surfactants (Tween 80 and Span 80) can result in similar physicochemical characteristics. Oral pharmacokinetic study of FEN Lf-SEDDS in a rat model resulted in 1.3 and 5.5 times higher relative bioavailability than marketed product and pure drug, respectively. The addition of lactoferrin could substitute synthetic surfactants in self-emulsifying drug delivery systems significantly.

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“…Tween and Lactoferrin can increase the FEN permeability through the intestinal epithelium. Surfactants also help bioavailability improvement by inhibiting pGP efflux transporter activity …”

Section: Resultsmentioning

confidence: 99%

Section: Selection Of Surfactant−cosurfactant By Pseudoternary Phase ...mentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Lactoferrin Reduces Surfactant Content in the Self-Emulsifying Drug Delivery System

Khairnar,

Jain,

Chatterjee

2024

ACS Omega

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“…The results are illustrated in Fig. 6 formulations could be attributed to the presence of its key component HS15, which has been shown to have a P-gp suppressing effect, thereby inhibiting the e ux of the P-gp substrate DOX [50]. However, further investigations are required to fully elucidate the precise mechanisms of DOXC 12 -LNC CL uptake by the cells.…”

Section: Doxc 12 -Lnc CL Show Superior Cytotoxicity Than Doxc 12 In G...mentioning

confidence: 96%

Local delivery of Doxorubicin prodrug via lipid nanocapsule-based hydrogel for the treatment of glioblastoma

Wang

Bergès

Malfanti

et al. 2023

Preprint

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Glioblastoma (GBM) recurrences appear in most cases around the resection cavity borders and arise from residual GBM cells that cannot be removed by surgery. Here, we propose a novel treatment that combines the advantages of nanomedicine and local drug delivery to target these infiltrating GBM cells. We developed an injectable lipid nanocapsules (LNC)-based formulation loaded with lauroyl-doxorubicin prodrug (DOXC12). Firstly, we demonstrated the efficacy of intratumoral administration of DOXC12 in GL261-GBM-bearing mice, which extended mice survival. Then, we formulated an injectable hydrogel by mixing the appropriate amount of prodrug with the lipophilic components of LNC. We optimized the hydrogel by incorporating cytidine-C16 (Cyt-C16) to achieve a mechanical stiffness adapted for an application in the brain post-surgery (DOXC12-LNCCL). DOXC12-LNCCL exhibited high DOXC12 encapsulation efficiency (95%) and a size of approximately 60 nm with sustained drug release in vitro for over 1 month. DOXC12-LNCCL exhibited enhanced cytotoxicity compared to free DOXC12 (IC50 of 49 and 89 nM, respectively) on GL261 GBM cells and prevented growth of GL261 spheroids cultured on organotypic brain slices. In vivo, post-surgical treatment with DOXC12-LNCCL significantly improved the survival of GL261-bearing mice. The combination of this local treatment with the systemic administration of anti-inflammatory drug ibuprofen further delayed the onset of recurrences. In conclusion, our study presents a promising therapeutic approach for the treatment of GBM. By targeting residual GBM cells and reducing the inflammation post-surgery, we present a new strategy to delay the onset of recurrences in the gap period between surgery and standard of care therapy.

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“…The lipophilic nature of LNC plays an important role in the uptake and absorption enhancement of poorly soluble drugs, increasing their bioavailability. [ 8 ] Moreover, the LNC shell's Solutol® HS15 permits the P‐gp inhibition efflux pump [ 9 ] expanding the range of drugs that can be delivered by the BBB.…”

Section: Introductionmentioning

confidence: 99%

Novel radioiodinated desvenlafaxine‐loaded lipid nanocapsule for brain delivery

Ayoub,

Abdel‐Mottaleb,

Ibrahem

et al. 2023

Archiv der Pharmazie

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Lipid nanocapsules (LNCs) are lipid nanocarriers developed for drug delivery enhancement. The antidepressant drug desvenlafaxine (DSV) was entrapped in LNC to improve its brain delivery. Different DSV‐loaded LNCs formulae using different oils and surfactants were studied to obtain the optimum formula for further studies. In vivo biodistribution studies were done using Swiss albino mice by intravenous injection of DSV‐loaded LNCs by radioiodination technique. The optimum DSV‐loaded LNC formula was obtained by using Labrafil® M1944CS as the oil and Solutol® HS15 as the surfactant in the ratio of 1:1, with a particle size of 34.28 ± 0.41 nm, a polydispersity index of 0.032 ± 0.05, a zeta potential of −25.77 ± 1.41, and good stability for up to 6 months. The in vivo biodistribution and pharmacokinetics data ensure the bioavailability improvement for DSV brain delivery as Cmax and AUC(1–t) increased more than double for intravenously DSV‐loaded LNCs compared with the DSV solution. In conclusion, the results obtained from this study give an insight into the great potential of using DSV‐loaded LNC for the enhancement of brain delivery.

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Non-ionic Surfactants as a P-Glycoprotein(P-gp) Efflux Inhibitor for Optimal Drug Delivery—A Concise Outlook

Cited by 23 publications

References 111 publications

Lactoferrin Reduces Surfactant Content in the Self-Emulsifying Drug Delivery System

Lactoferrin Reduces Surfactant Content in the Self-Emulsifying Drug Delivery System

Local delivery of Doxorubicin prodrug via lipid nanocapsule-based hydrogel for the treatment of glioblastoma

Novel radioiodinated desvenlafaxine‐loaded lipid nanocapsule for brain delivery

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