Studies on the encapsulation of diclofenac in small unilamellar liposomes of soya phosphatidylcholine

The purpose of the current study was to develop tizanidine HCl (TIZ; a myotonolytic agent used for treatment of spasticity) loaded nanotransfersomes intended for rectal administration, aiming to bypass the hepatic first-pass metabolism. TIZ-loaded nanotransfersomes were prepared by thin-film hydration method followed by characterization for various parameters including entrapment efficiency, vesicle diameter, in vitro release and ex vivo permeation studies. Transfersomal formulation composed of phosphatidylcholine and Tween 80 at a weight ratio of (85:15) gave a satisfactory results. It exhibited encapsulation efficiency of 52.39%, mean diameter of 150.33 nm, controlled drug release over 8 h and good permeation characteristics. Optimum formula was then incorporated into Pluronic-based thermoreversible gel using hydroxypropyl methylcellulose (HPMC) as a mucoadhesive polymer. Pharmacokinetic study was performed by rectal administration of transfersomes-loaded in situ gel to rabbits and compared with oral drug solution and rectal TIZ in situ gel. The pharmacokinetic study revealed that the transfersomal formulation successively enhanced the bioavailability of TIZ by about 2.18-fold and increased t 1/2 to about 10 h as compared to oral solution. It can be concluded that encapsulation of TIZ into nanotransfersomes can achieve a dual purpose of prolonged TIZ release and enhanced bioavailability and so may be considered as a promising drug delivery system for the treatment of spasticity.

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“…Being hydrophilic, TIZ would be incorporated into the internal aqueous core of vesicles as suggested by Lopes et al (2004). DOI: 10.1080DOI: 10.…”

Section: Entrapment Efficiencymentioning

confidence: 99%

Nanotransfersomes-loaded thermosensitive in situ gel as a rectal delivery system of tizanidine HCl: preparation, in vitro and in vivo performance

2017

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“…Liposomal gel was taken in beaker and spindle was dipped in it. The reading was measured at upper, middle and lower case at different intervals (Lopes et al 2004;Dave et al 2010).…”

Section: Viscositymentioning

confidence: 99%

Herbal liposome for the topical delivery of ketoconazole for the effective treatment of seborrheic dermatitis

et al. 2017

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The aim of the present study was to develop liposomal gel containing ketoconazole and neem extract for the treatment of seborrheic dermatitis in an effectual means. Azoles derivatives that are commonly used to prevent superficial fungal infections include triazole category like itraconazole. These drugs are available in the form of oral dosage that required a long period of time for treatment. Ketoconazole is available in the form of gel but is not used with any herbal extract. Neem (Azadirachta indica) leaves show a good anti-bacterial and anti-fungal activity and have great potential as a bioactive compound. The thin film hydration method was used to design an herbal liposomal preparation. The formulation was further subjected to their characterization as particle size, zeta potential, entrapment efficiency, % cumulative drug release, and anti-fungal activity and it was also characterized by the mean of their physicochemical properties such as FTIR, SEM, DSC, TGA, and AFM. The results show that the formulation of liposomes with neem extract F12 were found to be optimum on the basis of entrapment efficiency in the range 88.9 ± 0.7%, with a desired mean particle size distribution of 141.6 nm and zeta potential -45 mV. The anti-fungal activity of liposomal formulation F12 was carried out against Aspergillus niger and Candida tropicalis by measuring the inhibition zone 8.9 and 10.2 mm, respectively. Stability of optimized formulation was best seen at refrigerated condition. Overall, these results indicated that developed liposomal gel of ketoconazole with neem extract could have great potential for seborrheic dermatitis and showed synergetic effect for the treatment.

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“…A previous study suggests that interaction of DS with PC may adversely affect the structure and hence stability of the liposomes [16]. It was also observed that the liposomes were less stable the higher the proportion of PC, and more stable the higher the proportion of palm oil fractions.…”

Section: Discussionmentioning

confidence: 65%

“…This might be due to interactions between the lipid layers of liposome with DS. This is according to finding of Lopes which stated due to interaction of DS anion with the ammonium group of PC, the size of liposome that entraps DS reduced significantly, as the drug incorporated into the liposome [16]. Furthermore, large standard deviations found for mean particle size may be due to the broad heterogeneous sizes of the liposome.…”

Section: Discussionmentioning

confidence: 88%

Characterization of Diclofenac Liposomes Formulated with Palm Oil Fractions

Sabeti¹,

Ibrahim²,

Javar

et al. 2014

Trop. J. Pharm Res

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Studies on the encapsulation of diclofenac in small unilamellar liposomes of soya phosphatidylcholine

Cited by 64 publications

References 31 publications

Nanotransfersomes-loaded thermosensitive in situ gel as a rectal delivery system of tizanidine HCl: preparation, in vitro and in vivo performance

Nanotransfersomes-loaded thermosensitive in situ gel as a rectal delivery system of tizanidine HCl: preparation, in vitro and in vivo performance

Herbal liposome for the topical delivery of ketoconazole for the effective treatment of seborrheic dermatitis

Characterization of Diclofenac Liposomes Formulated with Palm Oil Fractions

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