Studies on a high encapsulation of colchicine by a niosome system

Hao, Yongmei; Zhao, Feiyang; Li, Na; Yang, Yanhong; Li, Kèan

doi:10.1016/s0378-5173(02)00301-0

Cited by 312 publications

(180 citation statements)

References 25 publications

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“…T80 being hydrophilic surfactant with high HLB value of 15 compared to 4.3 in case of the hydrophobic Sp 80, this probably elucidates the lower entrapment efficiency of T80 compared to Sp 80 formulations as previously discussed (Hao et al, 2002). Brij surfactants are polyoxyethylene alkyl ethers that differ in the number of hydrophilic oxyethylene groups and length of hydrophobic alkyl chain.…”

Section: Entrapment Efficiency (Ee%)mentioning

confidence: 79%

Ocular ketoconazole-loaded proniosomal gels: formulation, ex vivo corneal permeation and in vivo studies

2017

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Context: Vesicular drug carriers for ocular delivery have gained a real potential. Proniosomal gels as ocular drug carriers have been proven to be an effective way to improve bioavailability and patient compliance. Objective: Formulation and in vitro/ex vivo/in vivo characterization of ketoconazole (KET)-loaded proniosomal gels for the treatment of ocular keratitis. Materials and methods: The effect of formulation variables; HLB value, type and concentration of non-ionic surfactants (Tweens, Spans, Brijs and Pluronics) with or without lecithin on the entrapment efficiency (EE%), vesicle size and in vitro KET release was evaluated. An ex vivo corneal permeation study to determine the level of KET in the external eye tissue of albino rabbits and an in vivo assessment of the level of KET in the aqueous humors were performed. Results and discussion: In vivo evaluation showed an increase in bioavailability up to 20-folds from the optimum KET proniosomal gel formula in the aqueous humor compared to drug suspension (KET-SP). The selected formulae were composed of spans being hydrophobic suggesting the potential use of a more hydrophobic surfactant as Span during the formulation of formulae. Factors that stabilize the vesicle membrane and increase the entrapment efficiency of KET (namely low HLB, long alkyl chain, high phase transition temperature) slowed down the release profile. Conclusions: Proniosomal gels as drug delivery carriers were proven to be a promising approach to increase corneal contact and permeation as well as retention time in the eye resulting in a sustained action and enhanced bioavailability.

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Section: Entrapment Efficiency (Ee%)mentioning

confidence: 79%

Ocular ketoconazole-loaded proniosomal gels: formulation, ex vivo corneal permeation and in vivo studies

2017

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“…(25). It was also reported that Span forms hydrogen bond with the amido group of colchicines (17). This might also lead to better retention in elastic liposomes.…”

Section: Characteristics Of Elastic Liposomes Of Colchicinementioning

confidence: 91%

“…The maximum entrapment efficiency obtained was 66.3±2.2% for elastic liposomes (ELP20), 33.4±2.8% for liposomes, and 31.6±1.4% for niosome formulation, respectively. Colchicine is a highly hydrophilic drug, and its entrapment efficiency has been reported to be only 30% in conventional liposomal formulation (17). The higher entrapment efficiency in elastic liposomes can be attributed to the presence of higher lipid content and surfactant Span 80 in these vesicles.…”

Section: Characteristics Of Elastic Liposomes Of Colchicinementioning

confidence: 99%

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Elastic Liposomal Formulation for Sustained Delivery of Colchicine: In Vitro Characterization and In Vivo Evaluation of Anti-gout Activity

Singh

Utreja

Tiwary

et al. 2009

AAPS J

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Abstract. Colchicine, an alkaloid found in extracts of the plants Colchicum autumnale and Gloriosa superb, is effective in the treatment of acute gout and dermatological conditions like leuko-cytoclastic vasculitis, psoriasis, and Sweet's syndrome. Oral administration of colchicine is associated with gastrointestinal side effects and its accumulation in the body leads to bone marrow suppression. In the present study, an attempt has been made for development and in vitro and in vivo evaluation of elastic liposomal formulation for topical delivery of colchicine. The in vitro skin permeation study across rat skin found transdermal flux for different elastic liposomal formulations to range between 32.8±1.2 and 44.4± 1.9 μg h −1 cm −2 , which was approximately seven to 11 times higher than obtained using drug solution (4.3± 0.6 μg h −1 cm −2 ). The results of skin deposition study showed that elastic liposomal formulation provide 12.5-fold higher skin deposition as compared to drug solution of colchicine. Confocal laser scanning microscopy also revealed better accumulation and deeper penetration (up to 200 μm) of elastic liposomes than drug solution (up to 12 μm). The biological evaluation of various vesicular formulations and drug solution was carried out using monosodium urate-induced air pouch model. The results of anti-gout activity in rats showed better and sustained biological effects in 24 h measured in terms of exudate volume (63.1± 5.7% and 9.6±0.5% reduction with elastic liposomes and drug solution, respectively), reduction in leukocyte count (74.2±6.0% and 4.1±0.3% reduction with elastic liposomes and drug solution, respectively), decrease in inflammatory cells accumulation, and collagen deposition with elastic liposomal formulation than drug solution. Hence, the present study reveals that elastic liposomal formulation of colchicine possesses greater potential to enhance skin accumulation, prolong drug release, and improve the site-specificity of colchicine.

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“…The results presumably due to among these non-ionic surfactants, only Span80 has an unsaturated alkyl chain with strong hydrophile ability. Then, the adjacent molecule cannot be tight and is likely to be unstable in thermodynamics forming the coil-like flocculation (Hao et al, 2002). Furthermore, it was also suggested that PEGylated niosomes are not generally formed between hydrophile-lipophile-balance (HLB) of 14-17 (Uchegbu & Vyas, 1998) (Tweens excepted (Marzio et al, 2011)).…”

Section: Effects Of Non-ionic Surfactants Structure To Pegylated Niosmentioning

confidence: 99%

PEGylated non-ionic surfactant vesicles as drug delivery systems for Gambogenic acid

et al. 2013

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Gambogenic acid (GNA), a popular Chinese traditional medicine, has its limitations of coming into use due to its low aqueous solubility and poor bioavailability. In this study, therefore, the PEGylated non-ionic surfactant vesicles drug delivery systems were prepared from biocompatible non-ionic surfactant of Span60, cholesterol and dicetyl phosphate (DCP) by the improved ethanol injection method, and were modified with a polyethylene glycol monostearate15 (PEG15-SA). PEG15-SA, as a biocompatible, non-toxic and non-immunogenic hydrophilic segment, was grafted onto the surface of colloidal niosomes carries to reduce the uptake by the reticuloendothelial system (RES), prolonging the circulation time and attaining higher entrapment efficiency. To our knowledge, this work is the first to report that PEG15-SA was applied to coating of niosomes for encapsulation of GNA. The optimized PEG-GNA-NISVs (P-GNA-NISVs) were characterized in terms of mean vesicles size, polydispersity index (PDI), Zeta potential and entrapment efficiency of the P-GNA-NISVs. The results showed that the mean diameter, PDI, Zeta potential, and the entrapment efficiency of the P-GNA-NISVs were 70.1 nm, 0.166, À44.3 mV and 87.74%, respectively. Furthermore, the release studies of GNA from PEGylated niosomes in vitro and the pharmacokinetics in vivo exhibited a prolonged release profile as studied over 24 h. In conclusion, the result suggests that P-GNA-NISVs prepared in this way not only have higher encapsulation capacity, more colloidal stability but also offer an approach that the PEGylated niosomes is a promising carrier for anticancer GNA.

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Studies on a high encapsulation of colchicine by a niosome system

Cited by 312 publications

References 25 publications

Ocular ketoconazole-loaded proniosomal gels: formulation, ex vivo corneal permeation and in vivo studies

Ocular ketoconazole-loaded proniosomal gels: formulation, ex vivo corneal permeation and in vivo studies

Elastic Liposomal Formulation for Sustained Delivery of Colchicine: In Vitro Characterization and In Vivo Evaluation of Anti-gout Activity

PEGylated non-ionic surfactant vesicles as drug delivery systems for Gambogenic acid

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