Elastic Liposomal Formulation for Sustained Delivery of Antimigraine Drug: In Vitro Characterization and Biological Evaluation

Garg, Twinkal; Jain, Subheet Kumar; Singh, Harmanpreet; Sharma, Ajay; Tiwary, Ashok K.

doi:10.1080/03639040801965079

Cited by 28 publications

(31 citation statements)

References 30 publications

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“…However, the effectiveness of a vesicular system is strongly dependent on its physicochemical characteristics, in particular its thermodynamic state. Deformable vesicles like elastic liposomes have been found to be more effective in enhancing drug transport as compared to rigid vesicles like conventional liposomes for number of drug molecules like dexamethasone (10), diclofenac (11), zidovudine (12), lamivudine (13), propranolol (14), and rizatriptan (15). It was found that high elasticity of these vesicles could facilitate drug transport across the skin as compared to vesicles with rigid membranes.…”

Section: Introductionmentioning

confidence: 97%

“…The amount of drug deposited in the skin was found to be ten times higher after 6, 12, and 24 h administration of elastic liposomes as compared to the drug solution, three-and fivefold higher than liposomal and niosomal formulations. The observed better skin accumulation of elastic liposomes could be attributed to the difference in the mechanism of drug transport across the skin from elastic liposomes and drug solution (12,15). In contrast to colchicine molecule, elastic liposome is too large to enter into the cutaneous blood circulation; they directly bypass the cutaneous capillary bed, cross over to the subcutaneous capillary bed and ER 2 enhancement ratio, it is the ratio of amount of drug deposited from formulation to drug solution; ER 3 enhancement ratio, it is the ratio of transdermal flux from formulation to drug solution then to the subcutaneous tissue where they act as depot and sustain the drug release.…”

Section: Skin Permeation and Deposition Studymentioning

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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Section: Introductionmentioning

confidence: 97%

Section: Skin Permeation and Deposition Studymentioning

confidence: 99%

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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“…The passive transdermal delivery of an elastic liposomal formulation of rizatriptan was evaluated in both in vitro and in vivo analyses. 20 Compared with a solution of rizatriptan, the elastic liposome formulation allowed for a drug deposition that was 10-fold higher with a sustained release through 24 hours and a 3-fold increase in biologic activity, suggesting a possible future option for delivery of migraine therapy. Similar to the Zelrix patch, the iontophoretic delivery of zolmitriptan is also currently under investigation.…”

Section: Transdermal Delivery Of Other Triptansmentioning

confidence: 99%

Transdermal Delivery of Sumatriptan for the Treatment of Acute Migraine

Pierce

2010

Neurotherapeutics

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Summary:Migraine is a common, multisymptom disorder that can severely impact the daily activities of migraineurs. Triptans (primarily sumatriptan) are the most commonly prescribed treatment for migraine and are considered a relatively safe and effective initial therapy. Unfortunately, current sumatriptan formulations (i.e., oral, nasal, subcutaneous) may be associated with limitations that can result in patients' delaying or avoiding treatment. For oral formulations, these limitations include difficulty in taking an oral medication due to the nausea and vomiting that often accompany migraine, and inconsistent absorption, whereas nasal and subcutaneous formulations may be associated with low bioavailability and an undesirable rate of adverse events, respectively. An alternative to current formulations is transdermal drug delivery, particularly iontophoresis. Transdermal delivery has several advantages over current formulations, including avoidance of the gastrointestinal tract, controlled and sustained delivery, and convenient administration. This article reviews the in vitro, in vivo, and preclinical data supporting the use of iontophoresis for the delivery of sumatriptan, as well as the recent clinical data for Zelrix (NuPathe Inc., Conshohocken, PA), an iontophoretic sumatriptan patch currently in phase III development for the treatment of migraine.

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“…A migraine is a neurological disease characterized with recurrent headache (typically existing for 4-72 h), accompanied with frequent nausea, headache, vomiting, photophobia, phonophobia, and gastric disturbances. 101,102 Triggering neuropeptides is responsible to produce painful inflammation in cranial vessels and the dura mater. 101 An episodic migraine is considered a precursor of chronic migraines.…”

Section: Drug Delivery To the Brain: Antimigraine And Antiparkinson Dmentioning

confidence: 99%

“…101,102 Triggering neuropeptides is responsible to produce painful inflammation in cranial vessels and the dura mater. 101 An episodic migraine is considered a precursor of chronic migraines. 102 Thus, migraines could be progressive and necessitate sustained-release formulations for treatment of the disorder.…”

Section: Drug Delivery To the Brain: Antimigraine And Antiparkinson Dmentioning

confidence: 99%

Elastic liposomes as novel carriers: recent advances in drug delivery

Hussain¹,

Singh²,

Sharma

et al. 2017

IJN

138

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Elastic liposomes (EL) are some of the most versatile deformable vesicular carriers that comprise physiologically biocompatible lipids and surfactants for the delivery of numerous challenging molecules and have marked advantages over other colloidal systems. They have been investigated for a wide range of applications in pharmaceutical technology through topical, transdermal, nasal, and oral routes for efficient and effective drug delivery. Increased drug encapsulation efficiency, enhanced drug permeation and penetration into or across the skin, and ultradeformability have led to widespread interest in ELs to modulate drug release, permeation, and drug action more efficiently than conventional drug-release vehicles. This review provides insights into the versatile role that ELs play in the delivery of numerous drugs and biomolecules by improving drug release, permeation, and penetration across the skin as well as stability. Furthermore, it provides future directions that should ensure the widespread use of ELs across all medical fields.

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Elastic Liposomal Formulation for Sustained Delivery of Antimigraine Drug: In Vitro Characterization and Biological Evaluation

Cited by 28 publications

References 30 publications

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

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

Transdermal Delivery of Sumatriptan for the Treatment of Acute Migraine

Elastic liposomes as novel carriers: recent advances in drug delivery

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