
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%). Confocal laser scanning microscopy confirmed the capability of the flourolabeled bilosomes to penetrate deep within the skin.
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. 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.
| Country | Approval Status | Regulatory Body | Notes |
|---|---|---|---|
| United States | Approved | FDA | Under Prescription-only medication |
| European Union | Approved | EMA | Marketed under various brand names |
| India | Approved | DCGI | Available OTC in some states |
| Australia | Pending Approval | TGA | Under review for OTC sale |
Surfactant Effects on Lipid-Based Vesicles Properties. 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.
| 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 |
Understanding the effect of surfactant properties 200mg sildenafil citrate is crit. 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. Generally, the size of vesicles decreases by increasing the surfactant concn., carbon chain length, the hydrophilicity of the surfactant head group, and the hydrophilic-lipophilic balance. can also lead to an increase in charge, which in turn reduces vesicle aggregation and enhances the stability of the system. The vesicles' entrapment efficiency not only depends on the surfactant properties but also on the encapsulated drug. For example, the encapsulation of a lipophilic drug could be enhanced by using a surfactant with a low hydrophilic-lipophilic balance value. Moreover, the membrane permeability of vesicles depends on the surfactant's carbon chain length and transition temp. In addn., surfactants have a clear influence on pharmacokinetics and pharmacodynamics such as sustaining drug release, enhancing the circulation time of vesicles, improving targeting and cellular uptake.
K.; Abu Lila, A. S. Tailoring of Novel Bile Salt Stabilized Vesicles for Enhanced Transdermal Delivery of Simvastatin: A New Therapeutic Approach against Inflammation. 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. 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. AAPS PharmSciTech 2018, 19, 2276– 2287, DOI: 10.1208/s12249-018-1019-yGoogle ScholarThere is no corresponding record for this reference. A. A.; Abd-Elsalam, W. H.; Al-Mahallawi, A. M. Fabrication of novel ultradeformable bilosomes for enhanced ocular delivery of terconazole: In vitro characterization, ex vivo permeation and in vivo safety assessment. 2016, 513, 688– 696, DOI: 10.1016/j.ijpharm.2016.10.006Google ScholarThere is no corresponding record for this reference. 38Mahmoud, T. M.; Nafady, M. M.; Farouk, H. O.; Mahmoud, D. M.; Ahmed, Y. M.; Zaki, R. M.; Hamad, D. S.
Novel Bile Salt Stabilized Vesicles-Mediated Effective Topical Delivery of Diclofenac Sodium: A New Therapeutic Approach for Pain and Inflammation. In Pharmaceuticals 2022, 15, 1106, DOI: 10.3390/ph15091106Google ScholarThere is no corresponding record for this reference.
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39Zafar, A.; Alruwaili, N. K.; Imam, S. S.; Hadal Alotaibi, N.; Alharbi, K.
S.; Afzal, M.; Ali, R.; Alshehri, S.; Alzarea, S. I.; Elmowafy, M. Bioactive Apigenin loaded oral nano bilosomes: Formulation optimization to preclinical assessment. 2021, 29, 269– 279, DOI: 10.1016/j.jsps.2021.02.003Google ScholarThere is no corresponding record for this reference. 40Duangjit, S.; Pamornpathomkul, B.; Opanasopit, P.; Rojanarata, T.; Obata, Y.; Takayama, K.; Ngawhirunpat, T.
S. A.; Unissa, R.; Elsewedy, H. 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. H. Investigating the potential of employing bilosomes as a novel vesicular carrier for transdermal delivery of tenoxicam. Role of the charge, carbon chain length, and content of surfactant on the skin penetration of meloxicam-loaded liposomes.
J. Nanomedicine 2014, 9, 2005– 2017, DOI: 10.2147/IJN.S60674Google ScholarThere is no corresponding record for this reference.
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. in vesicle bilayers and to study the elasticity of vesicle bilayers. 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. 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. 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. 41Trotta, M.; Peira, E.; Debernardi, F.; Gallarate, M. Elastic liposomes for skin delivery of dipotassium glycyrrhizinate.
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. 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. 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. 30Khafagy, E. S.; Almutairy, B. (Elsevier Science B.V.)The aim of this study was to evaluate the possibility of using liposomes for skin delivery of dipotassium glycyrrhizinate (KG), an anti-inflammatory agent lovegra sildenafil employed in treating acute and chronic dermatitis, and of formulating such liposomes in an oil-in-water emulsion (O/W). KG had emulsifying properties and the possibility of producing elastic liposomes was verified. soya lecithin (PC) or hydrogenated soya lecithin (HPC) mixed with KG in wt./wt.
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). Bilosomes vesicles are formed of bilayer membrane of non-ionic surfactant mols. Although, bilosomes have not been proposed for transdermal drug delivery, this carrier seems to have promising potential in this regard. 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. method and then passed through a high pressure homogenizer. Liposome size and entrapment efficiency were detd. and the interaction between KG and HPC was investigated using differential scanning calorimetry. Transepidermal permeation through intact pig skin and skin deposition of KG from liposomes and O/W emulsion contg.