Tailoring of Bilosomal Nanogel for Augmenting the Off-Label Use of Sildenafil Citrate in Pediatric Pulmonary HypertensionClick to copy article linkArticle link copied!
in vesicle bilayers and to study the elasticity of vesicle bilayers.
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Artificial Cells, Nanomedicine, and Biotechnology 2015, 43, 282– 290, DOI: 10.3109/21691401.2014.883401Google ScholarThere is no corresponding record for this reference. 24Prodduturi, S.; Sadrieh, N.; Wokovich, A. M.; Doub, W. H.; Westenberger, B. J.; Buhse, L.
3.2. Effect of Independent Factors on SDF-BS Characteristics
Transdermal delivery of fentanyl from matrix and reservoir systems: effect of heat and compromised skin. 2010, 99, 2357– 2366, DOI: 10.1002/jps.22004Google ScholarThere is no corresponding record for this reference. 25Elsayed, M. M.; Abdallah, O. Y.; Naggar, V.
3.7. Characterization of SDF-BS Gel
F.; Khalafallah, N. M. Deformable liposomes and ethosomes: mechanism of enhanced skin delivery. 2006, 322, 60– 66, DOI: 10.1016/j.ijpharm.2006.05.027Google Scholar25Deformable liposomes and ethosomes: Mechanism of enhanced skin deliveryElsayed, Mustafa M. A.; Abdallah, Ossama Y.; Naggar, Viviane F.; Khalafallah, Nawal M.International Journal of Pharmaceutics (2006), 322 (1-2), 60-66CODEN: IJPHDE; ISSN:0378-5173. Studies with the spin label probes 5-, 12- and 16-doxyl stearic acid (DSA) indicated that both the order parameter and the rotational correlation times increased when the doxyl group was positioned closer to the headgroup region. These findings indicate that the fluidity of membranes decreased near the headgroup region.
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Comparing 16-DSA incorporated in vesicle formulations with either 30 or 70 mol% showed no difference in alkyl chain mobility as was reflected by the order parameter. The rotational correlation times, however, showed a slowdown from 0.38 to 0.71 and 1.13 ns when the PEG-8-L molar content was decreased from 100 to 70 and 30 mol% for PEG-8-L:L-595:CS vesicles, resp.
What other information should I know?
S. Vardenafil-Loaded Bilosomal Mucoadhesive Sponge for Buccal Delivery: Optimization, Characterization, and In Vivo Evaluation. Polymers (Basel) 2022, 14, 4184, DOI: 10.3390/polym14194184Google ScholarThere is no corresponding record for this reference. A. Transdermal Delivery of Ondansetron Hydrochloride via Bilosomal Systems: In Vitro, Ex Vivo, and In Vivo Characterization Studies. Extrusion measurements indicated an increase in elasticity of vesicle bilayers as the molar content of PEG-8-L was increased from 10 to 90 mol%. Incorporation of cholesterol sulfate stabilizes vesicles and thereby, decreases the elasticity. The increased elasticity correlated excellent with a redn. In conclusion, these results demonstrate that when the molar content of the single chain non-ionic surfactant PEG-8-L in vesicles is increased the elasticity is enhanced and the rotational correlation time is reduced. The enhanced elasticity might contribute to an optimal design of vesicles as drug carriers for transdermal application. 34Abdallah, M. H.; Lila, A. S. A.; Unissa, R.; Elsewedy, H.
Brand names
(Elsevier Ltd.)Despite intensive research, the mechanisms by which vesicular systems deliver drugs into intact skin are not yet fully understood. In the current study, possible mechanisms by which deformable liposomes and ethosomes improve skin delivery of ketotifen under non-occlusive conditions were investigated. In vitro permeation and skin deposition behavior of deformable liposomes and ethosomes, having ketotifen both inside and outside the vesicles (no sepn. of free ketotifen), having ketotifen only inside the vesicles (free ketotifen sepd.) and having ketotifen only outside the vesicles (ketotifen soln. added to empty vesicles), was studied using rabbit pinna skin.
Q. How long do the effects last?
Results over the counter drugs containing sildenafil suggested that both the penetration enhancing effect and the intact vesicle permeation into the stratum corneum might play a role in improving skin delivery of drugs by deformable liposomes, under non-occlusive conditions, and that the penetration enhancing effect was of greater importance in case of ketotifen. Regarding ethosomes, results indicated that ketotifen should be incorporated in ethosomal vesicles for optimum skin delivery. Ethosomes were not able to improve skin delivery of non-entrapped ketotifen. B. Formulation of Niosomal Gel for Enhanced Transdermal Lornoxicam Delivery: In-Vitro and In-Vivo Evaluation.
More common
Drug Deliv 2018, 15, 122– 133, DOI: 10.2174/1567201814666170224141548Google ScholarThere is no corresponding record for this reference. Gels 2022, 8, 235, DOI: 10.3390/gels8040235Google ScholarThere is no corresponding record for this reference. 28Ahmed, S.; Kassem, M. A.; Sayed, S. Bilosomes as Promising Nanovesicular Carriers for Improved Transdermal Delivery: Construction, in vitro Optimization, ex vivo Permeation and in vivo Evaluation. S.; Elghamry, H. A.; Soliman, M. S. Brucine-Loaded Ethosomal Gel: Design, Optimization, and Anti-inflammatory Activity. AAPS PharmSciTech 2021, 22, 269, DOI: 10.1208/s12249-021-02113-8Google ScholarThere is no corresponding record for this reference. A.; Aburahma, M.
| Parameter | Value | Units | Notes |
|---|---|---|---|
| Absorption Rate | 45 | min | Time to peak plasma concentration |
| Peak Plasma Level | 15 | ng/mL | After application |
| Half-life | 4.2 | hours | Elimination half-life |
| Bioavailability | 25 | % | Compared to oral administration |
H. Investigating the potential of employing bilosomes as a novel vesicular carrier for transdermal delivery of tenoxicam. 2015, 485, 329– 340, DOI: 10.1016/j.ijpharm.2015.03.033Google Scholar35Investigating the potential of employing bilosomes as a novel vesicular carrier for transdermal delivery of tenoxicamAl-Mahallawi, Abdulaziz M.; Abdelbary, Aly A.; Aburahma, Mona H.International Journal of Pharmaceutics (Amsterdam, Netherlands) (2015), 485 (1-2), 329-340CODEN: IJPHDE; ISSN:0378-5173. (Elsevier B.V.)Bilosomes represent an evolving vesicular carrier that have been explored for oral vaccines delivery based on its ability to resist enzymes and bile salts in the gastrointestinal tract (GIT).
| Step | Procedure | Tips | Precautions |
|---|---|---|---|
| 1 | Clean and dry the application area | Use alcohol wipes for cleanliness | Avoid open wounds |
| 2 | Apply a small amount (about 0.5 g) evenly | Use applicator if provided | Do not overdose |
| 3 | Allow absorption for 10-15 minutes | Do not massage vigorously | Avoid bathing immediately after |
| 4 | Wash hands thoroughly afterward | Prevent inadvertent transfer to other areas | Keep out of reach of children |
Bilosomes vesicles are formed of bilayer membrane of non-ionic surfactant mols.
- The gel allows easier dose adjustment compared to fixed-dose tablets.
- Some patients prefer the non-invasive nature of gel application.
- Patient counseling addresses realistic expectations from topical sildenafil.
- Use on damaged skin should be strictly avoided to prevent systemic absorption spikes.
- Can be incorporated into broader male sexual health management.
- Clinical effectiveness depends on consistent and correct application.
- Discreet packaging aids in user privacy and compliance.
Although, bilosomes have not been proposed for transdermal drug delivery, this carrier seems to have promising potential in this regard.
What should I know about storage and disposal of this medication?
J. Nanomedicine 2020, 15, 9783– 9798, DOI: 10.2147/IJN.S278688Google ScholarThere is no corresponding record for this reference. 29Shukla, A.; Mishra, V.; Kesharwani, P. Bilosomes in the context of oral immunization: development, challenges and opportunities. Drug Discov Today 2016, 21, 888– 899, DOI: 10.1016/j.drudis.2016.03.013Google ScholarThere is no corresponding record for this reference.
Customers say
30Khafagy, E. S.; Almutairy, B. K.; Abu Lila, A. S. Tailoring of Novel Bile Salt Stabilized Vesicles for Enhanced Transdermal Delivery of Simvastatin: A New Therapeutic Approach against Inflammation.
How does sildenafil work (mechanism of action)?
Polymers (Basel) 2023, 15, 677, DOI: 10.3390/polym15030677Google ScholarThere is no corresponding record for this reference. 31Aldawsari, M. F.; Khafagy, E. S.; Alotaibi, H. F.; Abu Lila, A. Accordingly, the aim of this investigation was to assess the capability and safety of utilizing bilosomes for transdermal delivery of tenoxicam (TX) as a model drug. A 3122 full factorial design was adopted to study the effects of different formulation parameters on bilosomes properties and select the optimal formulation using Design-Expert software. The selected formulation displayed nano-sized spherical vesicles (242.5 ± 6.43 nm) with reasonable entrapment efficiency percent (68.33 ± 2.33%).
Cited By
AAPS PharmSciTech 2018, 19, 2276– 2287, DOI: 10.1208/s12249-018-1019-yGoogle ScholarThere is no corresponding record for this reference. A. Elasticity of vesicles assessed by electron spin resonance, electron microscopy and extrusion measurements. 2001, 217, 13– 24, DOI: 10.1016/S0378-5173(01)00576-2Google Scholar33Elasticity of vesicles assessed by electron spin resonance, electron microscopy and extrusion measurementsvan den Bergh, B. Fatty acid spin labels were incorporated into vesicles, composed of the single chain non-ionic surfactant octaoxyethylenelaurate-ester (PEG-8-L), the sucrose laurate-ester L-595 and cholesterol sulfate (CS) to monitor local dynamic properties of lipid mols. Confocal laser scanning microscopy confirmed the capability of the flourolabeled bilosomes to penetrate deep within the skin.
| Ingredient | Concentration | Purity (%) | Solvent Used | pH Level | Preservatives |
|---|---|---|---|---|---|
| Sildenafil Citrate | 10 mg/g | 99.5 | Propylene Glycol | 5.5 | Methylparaben |
| Glycerin | -- | -- | -- | -- | -- |
| Carbomer | 1.5% | -- | -- | -- | -- |
| Ethanol | 2% | -- | -- | -- | -- |
| Purified Water | q.s. to 100g | -- | -- | -- | -- |
Both, ex vivo permeation and in vivo skin deposition studies confirmed the superiority of bilosomes over drug soln. study proved the safety of topically applied bilosomes.
- Some clinical studies suggest sildenafil gel causes less headache than oral forms.
- Topical application reduces systemic blood concentrations, minimizing cardiovascular risks.
- The gel form is especially suitable for patients with gastrointestinal issues.
- Use with caution in patients with certain dermatological diseases.
- Consult a physician before switching from oral to topical sildenafil formulations.
- Regular follow-ups help adjust dosage and monitor effectiveness.
- Use in women is not well studied and generally not recommended.
In summary, the highlighted results confirmed that bilosomes can be further adopted for delivering drugs transdermally. 36Bnyan, R.; Khan, I.; Ehtezazi, T.; Saleem, I.; Gordon, S.; O’Neill, F.; Roberts, M. Surfactant Effects on Lipid-Based Vesicles Properties.
- Alternative delivery forms like gels provide options for personalized therapy.
- Patient preference studies show interest in topical vs oral ED treatments.
- The gel form may afford decreased systemic exposure and drug interactions.
- Education on gel use reduces misuse and increases effectiveness.
- Some formulations include preservatives to maintain product safety.
- Clinical review highlights benefits for patients with certain comorbidities.
- Not recommended for use in men under 18 years of age.
2018, 107, 1237– 1246, DOI: 10.1016/j.xphs.2018.01.005Google Scholar36Surfactant effects on lipid-based vesicles propertiesBnyan, Ruba; Khan, Iftikhar; Ehtezazi, Touraj; Saleem, Imran; Gordon, Sarah; O'Neill, Francis; Roberts, MatthewJournal of Pharmaceutical Sciences (Philadelphia, PA, United States) (2018), 107 (5), 1237-1246CODEN: JPMSAE; ISSN:0022-3549. Understanding the effect of surfactant properties is crit.
4. Conclusions
Transfersomes--a novel vesicular carrier for enhanced transdermal delivery: development, characterization, and performance evaluation. 2003, 29, 1013– 1026, DOI: 10.1081/DDC-120025458Google ScholarThere is no corresponding record for this reference. 20Singh, M. R.; Singh, D. K.; Saraf, S.
2.9. Ex Vivo Skin Permeation Studies
Development and in vitro evaluation of polar lipid based lipospheres for oral delivery of peptide drugs. 2009, 1, 15– 26, DOI: 10.5138/ijdd.2009.0975.0215.01002Google ScholarThere is no corresponding record for this reference. Enhancing Transdermal Delivery of Glimepiride Via Entrapment in Proniosomal Gel. Journal of Young Pharmacists 2016, 8, 335– 340, DOI: 10.5530/jyp.2016.4.8Google ScholarThere is no corresponding record for this reference. 22Richard, C.; Cassel, S.; Blanzat, M.
2.3. Design Optimization of SDF-Loaded Bilosomes
Vesicular systems for dermal and transdermal drug delivery. 2021, 11, 442– 451, DOI: 10.1039/D0RA09561CGoogle ScholarThere is no corresponding record for this reference. 23Singh, D.; Pradhan, M.; Nag, M.; Singh, M. R. Vesicular system: Versatile carrier for transdermal delivery of bioactives. This review evaluates previous studies to explain the influence of surfactant properties on the behavior of lipid vesicular systems, specifically their size, charge, stability, entrapment efficiency, pharmacokinetics, and pharmacodynamics.