&lt;p&gt;Spray-Dried Silica Xerogel Nanoparticles as a Promising Gastroretentive Carrier System for the Management of Chemotherapy-Induced Nausea and Vomiting&lt;/p&gt;

Ghoneim, Amira M.; Tadros, Mina Ibrahim; Alaa-Eldin, Ahmed Adel

doi:10.2147/ijn.s232841

Cited by 7 publications

(6 citation statements)

References 35 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Practically, the burst drug release is needed to rapidly achieve the minimum effective drug concentration, while the more prolonged drug release is required to maintain the therapeutic drug response for an extended period. 44 The drug release profile discriminators (Q 0.5h and Q 8h ; Y4 & Y5) of AGM-loaded invasomes are listed in Table 1 . Statistical analysis of data confirmed that the drug: lipid ratio (X1), terpene type (X2) and terpene concentration (X3) had significant impacts on Q 0.5h and Q 8h .…”

Section: Resultsmentioning

confidence: 99%

<p>Low-Frequency versus High-Frequency Ultrasound-Mediated Transdermal Delivery of Agomelatine-Loaded Invasomes: Development, Optimization and in-vivo Pharmacokinetic Assessment</p>

Tawfik¹,

Tadros²,

Mohamed³

et al. 2020

IJN

Self Cite

View full text Add to dashboard Cite

Aim Agomelatine (AGM) is the first melatonergic antidepressant. It suffers from low oral bioavailability (<5%) due to extensive hepatic metabolism. The current work aimed to develop an alternative AGM-loaded invasomes to enhance transdermal drug bioavailability. Methodology AGM-loaded invasomes were developed using two drug: lipid ratios (1:10 or 1:7.5), four terpene types (limonene, cineole, fenchone or citral) and two terpene concentrations (0.75% or 1.5%, w/v). They were characterized for drug entrapment efficiency (EE%), particle size (PS), zeta potential (ZP) and drug released percentages after 0.5h (Q 0.5h ) and 8h (Q 8h ). The optimum invasomes (I1, I2 and I4) were evaluated for morphology, drug-crystallinity, and ex-vivo drug flux. The variables influencing sonophoresis of the best achieved invasomal gel system (I2) were optimized including, ultrasound frequency (low, LFU or high, HFU), mode (pulsed or continuous), application period (10 min or 15 min) and duty cycle (50% or 100%). AGM pharmacokinetics were evaluated in rabbits following transdermal application of I2-LFU-C4 system, relative to AGM oral dispersion. Results The superiority of I2 invasomes [comprising AGM and phosphatidylcholine (1:10) and limonene (1.5% w/v)] was statistically revealed with respect to EE% (78.6%), PS (313 nm), ZP (−64 mV), Q 0.5h (30.1%), Q 8h (92%), flux (10.79 µg/cm2/h) and enhancement ratio (4.83). The optimum sonophoresis conditions involved application of LFU in the continuous mode for 15 min at a 100% duty cycle (I2-LFU-C4 system). The latter system showed significantly higher C max , and relative bioavailability (≈ 7.25 folds) and a similar T max (0.5 h). Conclusion I2-LFU-C4 is a promising transdermal system for AGM.

show abstract

Section: Resultsmentioning

confidence: 99%

<p>Low-Frequency versus High-Frequency Ultrasound-Mediated Transdermal Delivery of Agomelatine-Loaded Invasomes: Development, Optimization and in-vivo Pharmacokinetic Assessment</p>

Tawfik¹,

Tadros²,

Mohamed³

et al. 2020

IJN

Self Cite

View full text Add to dashboard Cite

show abstract

“…The in vitro drug release profiles from RLX-loaded PVA, RLX-loaded PVA/HPMC and RLX-loaded PVA/CS core-sheath NFs in PBS pH 6.8 with 0.1% tween at 37 • C in comparison to RLX aqueous dispersion, are displayed in Figure 4. Practically, the burst drug release is required in order to rapidly achieve the minimum effective drug concentration, while the prolonged drug release is required to maintain the therapeutic drug response for an extended period [67]. A fast release of the drug was observed with an initial burst release of formulae E3, E6, E9, E2, E8, E1, and E7.…”

Section: In Vitro Release Studiesmentioning

confidence: 99%

Green Nanotechnology in the Formulation of a Novel Solid Dispersed Multilayered Core-Sheath Raloxifene-Loaded Nanofibrous Buccal Film; In Vitro and In Vivo Characterization

et al. 2021

View full text Add to dashboard Cite

Green nanotechnology utilizes the principles of green chemistry to formulate eco-friendly nanocarrier systems to mitigate patients and environment hazards. Raloxifene (RLX) demonstrates poor aqueous solubility (BCS class II) and low bioavailability, only 2% (extensive first-pass metabolism). The aim of this study is to enhance RLX solubility and bioavailability via development of novel solid dispersed multilayered core-sheath RLX-loaded nanofibers (RLX-NFs) without the involvement of organic solvents. A modified emulsion electrospinning technique was developed. Electrospinning of an RLX-nanoemulsion (RLX-NE) with polymer solution (poly vinyl alcohol (PVA), hydroxypropyl methylcellulose (HPMC), and chitosan (CS) in different volume ratios (1:9, 2:8, and 4:6) using D-optimal response surface methodology was adopted. In vitro characterization of RLX-loaded NFs was performed; scanning electron microscope (SEM), thermal analysis, drug content, release studies, and bioadhesion potential. The optimum NFs formula was evaluated for morphology using high-resolution transmission electron microscopy (HRTEM), and ex vivo drug permeation. The superiority of E2 (comprising RLX-NE and PVA (2:8)) over other NF formulae was statistically observed with respect to Q60 (56.048%), Q240 (94.612%), fiber size (594.678 nm), mucoadhesion time 24 h, flux (5.51 µg/cm2/h), and enhancement ratio (2.12). RLX pharmacokinetics parameters were evaluated in rabbits following buccal application of NF formula E2, relative to RLX oral dispersion. E2 showed significantly higher Cmax (53.18 ± 4.56 ng/mL), and relative bioavailability (≈2.29-fold).

show abstract

“…It inhibits the vagus nerve from activating the vomiting center in the medulla oblongata [ 7 , 8 ]. GS is a water-soluble drug having a 3–4 h half-life in healthy volunteers and a 9–12 h half-life in cancer patients [ 9 ]. Consequently, it is necessary to extend the half-life of GS in cancer patients.…”

Section: Introductionmentioning

confidence: 99%

“…Furthermore, individuals with impaired swallowing ability or nausea symptoms may find it difficult to take GS tablets by mouth. It also has a limited oral bioavailability because of hepatic first-pass metabolism [ 9 ]. GS injection is an invasive dosage form; thus, driving patients to face needless pain and the risk of infection due to injection, which is a serious concern for immunocompromised people.…”

Section: Introductionmentioning

confidence: 99%

Intranasal Delivery of Granisetron to the Brain via Nanostructured Cubosomes-Based In Situ Gel for Improved Management of Chemotherapy-Induced Emesis

et al. 2022

View full text Add to dashboard Cite

This research aimed to boost granisetron (GS) delivery to the brain via the intranasal route to better manage chemotherapy-induced emesis. Glycerol monooleate (GMO), Poloxamer 407 (P 407) and Tween 80 (T 80) were used to formulate GS-loaded cubosomes (GS-CBS) utilizing a melt dispersion-emulsification technique. GS-CBS were characterized by testing particle diameter, surface charge and entrapment efficiency. The formulations were optimized using a Box–Behnken statistical design, and the optimum formula (including GMO with a concentration of 4.9%, P 407 with a concentration of 10%, and T 80 with a concentration of 1%) was investigated for morphology, release behavior, ex vivo permeation through the nasal mucosa, and physical stability. Moreover, the optimal formula was incorporated into a thermosensitive gel and subjected to histopathological and in vivo biodistribution experiments. It demonstrated sustained release characteristics, increased ex vivo permeability and improved physical stability. Moreover, the cubosomal in situ gel was safe and biocompatible when applied to the nasal mucosa. Furthermore, compared to a drug solution, the nose-to-brain pathway enhanced bioavailability and brain distribution. Finally, the cubosomal in situ gel may be a potential nanocarrier for GS delivery to the brain through nose-to-brain pathway.

show abstract

<p>Spray-Dried Silica Xerogel Nanoparticles as a Promising Gastroretentive Carrier System for the Management of Chemotherapy-Induced Nausea and Vomiting</p>

Cited by 7 publications

References 35 publications

<p>Low-Frequency versus High-Frequency Ultrasound-Mediated Transdermal Delivery of Agomelatine-Loaded Invasomes: Development, Optimization and in-vivo Pharmacokinetic Assessment</p>

<p>Low-Frequency versus High-Frequency Ultrasound-Mediated Transdermal Delivery of Agomelatine-Loaded Invasomes: Development, Optimization and in-vivo Pharmacokinetic Assessment</p>

Green Nanotechnology in the Formulation of a Novel Solid Dispersed Multilayered Core-Sheath Raloxifene-Loaded Nanofibrous Buccal Film; In Vitro and In Vivo Characterization

Intranasal Delivery of Granisetron to the Brain via Nanostructured Cubosomes-Based In Situ Gel for Improved Management of Chemotherapy-Induced Emesis

Contact Info

Product

Resources

About