The aim of this study was to investigate the presence of a possible direct correlation between vesicle elasticity and the amount of drug reaching the brain intranasally. Therefore, transfersomes were developed using phosphatidylcholine (PC) as the lipid matrix and sodium deoxycholate (SDC), Span® 60, Cremophor® EL, Brij® 58, and Brij® 72 as surfactants. The influence of the type of surfactant and PC-to-surfactant ratio on vesicle morphology, size, membrane elasticity, drug entrapment, and in vitro drug release was studied. The prepared transfersomes were mainly spherical in shape, with diameters ranging from 310 to 885 nm. Transfersomes containing SDC and Span 60 with optimum lipid-to-surfactant molar ratio showed suitable diameters (410 and 380 nm, respectively) and deformability indices (17.68 and 20.76 mL/sec, respectively). Values for absolute drug bioavailability in rat plasma for transfersomes containing SDC and those containing Span 60 were 24.75 and 51.35%, whereas AUC0–360min values in rat brain ...

Brain delivery of olanzapine by intranasal administration of transfersomal vesicles.

Transdermal absorption enhancement of papain loaded in elastic niosomes incorporated in gel for scar treatment

The objective of present work was to develop novel sunscreen creams containing polymeric nanoparticles (NPs) of morin. Polymeric NPs containing morin were prepared and optimized. The creams containing morin NPs were also prepared and evaluated. Optimized NPs exhibited particle size of 90.6 nm and zeta potential of −31 mV. The entrapment efficiency of morin, within the polymeric NPs, was found to be low (12.27%). Fourier transformed infrared spectroscopy and differential scanning calorimetry studies revealed no interaction between morin and excipients. Transmission electron microscopy and atomic force microscopy revealed that the NPs were spherical in shape with approximately 100 nm diameter. Optimized NPs showed excellent in vitro free radical scavenging activity. Skin permeation and deposition of morin from its NPs was higher than its plain form. Different sunscreen creams (SC1–SC8) were formulated by incorporating morin NPs along with nano zinc oxide and nano titanium dioxide. SC5 and SC8 creams showed excellent sun protection factor values (≈40). In vitro and in vivo skin permeation studies of sunscreen creams containing morin NPs indicated excellent deposition of morin within the skin. Morin NPs and optimized cream formulations (SC5 and SC8) did not exhibit cytotoxicity in Vero and HaCaT cells. Optimized sunscreen creams showed excellent dermal safety. SC5 and SC8 creams demonstrated exceptional in vivo antioxidant effect (estimation of catalase, superoxide dismutase, and glutathione) in UV radiation-exposed rats. The optimized sunscreen creams confirmed outstanding UV radiation protection as well as antioxidant properties.

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Development and evaluation of sunscreen creams containing morin-encapsulated nanoparticles for enhanced UV radiation protection and antioxidant activity.

Phospholipid membrane tubulation using ceramide doping “Cerosomes”: Characterization and clinical application in psoriasis treatment

Context: A transdermal delivery system is warranted for repaglinide (RPG) which possesses half-life of 1 h and oral bioavailability of 56%. Ethosomes are useful tools for transdermal drug delivery.Objectives: To prepare and evaluate ethosomes as mode for transdermal delivery of RPG.Material and methods: Ethosomes loaded with RPG were prepared from dipalmitoyl phosphatidylcholine and ethanol by the cold method. They were characterized using Fourier transform infrared spectroscopy and differential scanning calorimetry. They were evaluated for vesicle size, entrapment efficiency and ex-vivo skin permeation. Ethosomal composition was optimized using the 32 factorial design. Gel containing optimzsed ethosomes was studied for antidiabetic activity in rats.Result: RPG ethosomes possessing the size of 0.171–1.727 µm and entrapment efficiency of 75–92% were obtained. They demonstrated a significantly higher permeation (64–97% of the administered dose) across excised rat skin when compared to free drug and ...

A study on ethosomes as mode for transdermal delivery of an antidiabetic drug.

The aim of the present study was to investigate the potential of transfersomal formulations for transdermal delivery of indinavir sulfate and to evaluate Span 80, Tween 80, Sodium cholate and Sodium deoxycholate as edge activators. Vesicles containing phosphatidylcholine (PC) mixed with edge activators and indinavir sulfate were prepared by conventional rotary evaporation method and characterized for various parameters including vesicles shape and surface morphology, size and size distribution, entrapment efficiency, elasticity, turbidity, and in vitro drug release. The compositions of refined formulations were predicted, liposomes prepared, and tested against control. Skin permeation profile of transfersomal formulation bearing indinavir sulfate was observed and the investigations revealed an enhanced transdermal flux (8.91±0.9 µg/cm2 /hr) and decrease lag time (0.9 hr) for indinavir sulfate. The obtained flux was nearly 7.5 and 12.04 times higher than conventional liposomal formulation bearing indinavir sulfate and plain drug solution. These results suggested that transfersomes are potential vehicles for improved transdermal delivery of indinavir sulfate and Span 80, Tween 80 and Sodium cholate were equivalent to Sodium deoxycholate as edge-activators.

Enhanced Transdermal Delivery of Indinavir Sulfate Via Transfersomes

The present work was envisaged to reduce the dosing frequency and improve patient compliance by designing and evaluating Sustained Release Mucoadhesive (SRM) microspheres of Metformin hydrochloride (MH) for effective control of diabetes type-2. Microspheres were prepared by emulsification solvent evaporation method using Sodium carboxy methyl cellulose (SCMC), Carbopol 934P (CP), and Hydroxyl propyl methyl cellulose K4M (HPMC) as a mucoadhesive polymers. Microspheres prepared were found discrete, spherical and free flowing. The microspheres exhibits good mucoadhesive properties and showed high drug entrapment efficiency. MH release from these microspheres was slow and extended and dependent on the type of polymer used. The mean particle size decreased and the drug release rate increased at higher Stirring speed of emulsion content. Among all the formulation, formulation F1 containing SCMC and F2 containing CP showed the best reproducible results and mucoadhesive profile with good surface morphology. The data obtained thus suggest that mucoadhesive microspheres can successfully design for sustained delivery of MH and to improve patient compliance.

https://papers.ssrn.com/sol3/Delivery.cfm/SSRN_ID3774725_code4562211.pdf?abstractid=3774725&mirid=1

Design and Evaluation of SRM Microspheres of Metformin Hydrochloride

The aim of the present study is to investigate the potential of ethosomal formulations for transdermal delivery of indinavir sulphate from ethosomes. Vesicles containing phosphatidylcholine mixed with ethanol and indinavir sulphate were prepared by conventional mechanical stirrer method and characterized by various parameters (vesicles shape and surface morphology, size and size distribution, entrapment efficiency, elasticity, turbidity and in vitro drug release). The effect of different formulation variable on skin permeation of indinavir sulphate was studied via synthetic semipermeable membrane or skin of new born mice by using diffusion cell. The selected system were incorporated into carbopol 934P gel and evaluated for both drug permeation and mice skin deposition. The optimized ethosomal formulation showed transdermal flux of 25.01±0.34 μg/cm2 /h across rat skin as compared to 2.98±0.21μg/cm2 /h for plane drug solution, 4.28±0.54 μg/cm2 /h for hydroethanolic solution and 9.7±0/21 μg/cm2 /h for classical liposomes. The obtained flux was nearly 7.5 and 12.04 times higher than conventional liposomal formulation bearing indinavir sulphate and plain drug solution. These results suggest that ethosomes are potential vehicles for improved transdermal delivery of indinavir sulphate.

Enhancement of Transdermal Permeation of Indinavir Sulfate via EthosomeVesicles

The aim of the present study is to investigate the potential of ethosomal formulations for transdermal delivery of indinavir sulphate from ethosomes. Vesicles containing phosphatidylcholine mixed with ethanol and indinavir sulphate were prepared by conventional mechanical stirrer method and characterized by various parameters (vesicles shape and surface morphology, size and size distribution, entrapment efficiency, elasticity, turbidity and in vitro drug release). The effect of different formulation variable on skin permeation of indinavir sulphate was studied via synthetic semipermeable membrane or skin of new born mice by using diffusion cell. The selected system were incorporated into carbopol 934P gel and evaluated for both drug permeation and mice skin deposition. The optimized ethosomal formulation showed transdermal flux of 25.01±0.34 μg/cm 2 /h across rat skin as compared to 2.98±0.21μg/cm 2 /h for plane drug solution, 4.28±0.54 μg/cm 2 /h for hydroethanolic solution and 9.7±0/21 μg/cm 2 /h for classical liposome s. The obtained flux was nearly 7.5 and 12.04 times higher than conventional liposomal formulation bearing indinavir sulphate and plain drug solution. These results suggest that ethosomes are potential vehicles for improved transdermal delivery of indinavir sulphate.

Shweta Aggarwal

Papers

Enhanced Transdermal Delivery of Indinavir Sulfate Via Transfersomes

Design and Evaluation of SRM Microspheres of Metformin Hydrochloride

Enhancement of Transdermal Permeation of Indinavir Sulfate via EthosomeVesicles

Enhancement of Transdermal Permeation of Indinavir Sulfate via EthosomeVesicles