A COMPARATIVE STUDY OF TERBINAFINE ETHOSOMAL FORMULATIONS: A NOVEL APPROACH

AbstractThe present research work aimed at the impact of reduced vesicular size on the characteristics of ethosomes by comparing with the regular vesicular size of ethosomes as topical drug delivery vehicle to achieve optimal localized drug concentration and reduced dose frequency of the Terbinafine hydrochloride (TH), an antifungal drug. Oral use of TH contraindicated resulting from sever side effect, thus topical administration is recommended. Commercially available TH creams, lotions and sprays, have limitation of relatively short residual period at target site. The entrapment of drug in vesicles improves localization, solubility and availability of drug at the site; resulting in reduction of the dose. Ethosomes containing drug were prepared by employing higher concentration of alcohol in the form of hydroalcoholic or hydroglycolic phospholipid. Sonicated and unsonicated ethosomes were investigated for shape, particle size, and entrapment efficiency. Electronic microscope investigation not only revealed, vital evidence for presence of phospholipid vesicles in TH ethosomal systems but also displayed greater uniformity in size and shape of sonicated ethosomes than unsonicated ethosomes. Furthermore, the Comparative investigation was carried out for ex vivo skin permeation, ex vivo drug release and entrapment efficiency studies. Drug release followed zero order release rate kinetics. Drug accumulation study showed more than 19.01 % of drug was deposited into skin by sonicated ethosomal formulation as compared to 2.57 % by unsonicated ethosomal formulation. Sonicated and unsonicated ethosomes were found stable at refrigeration and room temperature conditions during stability studies. Drug accumulation studies in deep skin strata was found to be comparatively greater in sonicated ethosomes, which indicates higher localized drug and that in turn reduces dose frequency.

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Design and Evaluation of Long Acting Biodegradable PLGA Microspheres for Ocular Drug Delivery

Nanoscience &Nanotechnology-Asia ◽

10.2174/2210681210666191223144755 ◽

2019 ◽

Vol 10 ◽

Author(s):

Anjali Pandya ◽

Rajani Athawale ◽

Durga Puro ◽

Geeta Bhagwat

Keyword(s):

Particle Size ◽

Drug Release ◽

Degradation Products ◽

Ex Vivo ◽

Research Work ◽

Entrapment Efficiency ◽

Rational Approach ◽

Plga Microspheres ◽

Long Acting

Background: The research work involves development of PLGA biodegradable microspheres loaded with dexamethasome for intraocular delivery. Objective: To design and evaluate long acting PLGA microspheres for ocular delivery of dexamethasone. Method: Present formulation involves the development of long acting dexamethasone loaded microspheres composed of a biodegradable controlled release polymer, Poly(D, L- lactide-co-glycolide) (PLGA), for the treatment of posterior segment eye disorders intravitreally. PLGA with monomer ratio of 50:50 of lactic acid to glycolic acid was used to achieve a drug release up to 45 days. Quality by Design approach was utilized for designing the experiments. Single emulsion solvent evaporation technique along with high pressure homogenization was used to facilitate formation of microspheres. Results: Particle size evaluation, drug content and drug entrapment efficiency were determined for the microspheres. Particle size and morphology was observed using Field Emission Gun-Scanning Electron Microscopy (FEG-SEM) and microspheres were in the size range of 1-5 μm. Assessment of drug release was done using in vitro studies and transretinal permeation was observed by ex vivo studies using goat retinal tissues. Conclusion: Considering the dire need for prolonged therapeutic effect in diseases of the posterior eye, an intravitreal long acting formulation was designed. Use of biodegradable polymer with biocompatible degradation products was a rational approach to achieve this aim. Outcome from present research shows that developed microspheres would provide a long acting drug profile and reduce the frequency of administration thereby improving patient compliance.

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Development and Characterization of Apremilast Transethosomal Gel for Transdermal Delivery

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2021.14.3.8 ◽

2021 ◽

Vol 14 (3) ◽

pp. 5508-5518

Author(s):

Mrunal Rahangdale ◽

Prachi Pandey

Keyword(s):

Drug Release ◽

Sustained Release ◽

Ex Vivo ◽

Skin Permeation ◽

Entrapment Efficiency ◽

Oral Route ◽

Tem Analysis ◽

Vesicle Size ◽

Ex Vivo Permeation ◽

Permeation Studies

The apremilast is anti-inflammatory drug and PDE-4 inhibitor, used in treatment of psoriasis. The oral route of apremilast has limitation of GI irritation and frequent dosage regimen.The objective of the present work was aimed to prepare transethosomal gel of apremilast to achieve more skin permeation, more drug entrapment efficiency and sustained release. The transethosome vesicle containing apremilast was prepared by using Rotary vacuum evaporator, followed by probe sonication. The Box-Behnken design was used to optimize the formulation by taking quantity of lipoid S 100, sodium cholate and ethanol as independent variable and vesicle size, entrapment efficiency and cumulative drug release as dependent variable. The optimized batch of transethosome vesicle was incorporated in 1 % of Carbopol gel base. The prepared optimized batch was evaluated for size, zeta potential, surface morphology, pH, viscosity, spreadability, extrudability, drug content and ex-vivo permeation studies. The result showed that optimized batch of transethosome was found to have vesicle size of 130.8 nm, entrapment efficiency of 62.83 % and cumulative drug release of gel 73.13 %. The transethosome vesicles were found to be spherical and uniform in size based on TEM analysis. The ex-vivo permeation studies were performed for 24 hrs through the rat skin. The formulation was found to show better skin permeation and sustained release. The formulation showed satisfactory result with respect to pH, gel characteristics and stability. Thus, can concluded that transethosomal gel containing apremilast could be an effective option for treatment of psoriasis.

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Formulation and Optimization of Nanospanlastics for Improving the Bioavailability of Green Tea Epigallocatechin Gallate

Pharmaceuticals ◽

10.3390/ph14010068 ◽

2021 ◽

Vol 14 (1) ◽

pp. 68

Author(s):

Eman A. Mazyed ◽

Doaa A. Helal ◽

Mahmoud M. Elkhoudary ◽

Ahmed G. Abd Elhameed ◽

Mohamed Yasser

Keyword(s):

Drug Release ◽

Pharmacokinetic Study ◽

Ex Vivo ◽

Epigallocatechin Gallate ◽

Entrapment Efficiency ◽

Sustained Drug Release ◽

Ethanol Injection ◽

23 Factorial Design ◽

The Impact

The present study aimed to investigate the potential of nanospanlastics for boosting the bioavailability of epigallocatechin gallate (EGCG). EGCG has valuable effects like anti-inflammation, anti-oxidation, and anti-tumorigenesis. Unfortunately, it has a low oral bioavailability due to its limited permeation and poor stability. To overcome these pitfalls, EGCG was fabricated as a nanospanlastic. Nanospanlastics are flexible nanovesicles that are composed of surfactants and edge activators (EAs). EAs improve the deformability of spanlastics by acting as a destabilizing factor of their vesicular membranes. EGCG-loaded spanlastics were prepared by an ethanol injection method, according to 23 factorial design, to explore the impact of different independent variables on entrapment efficiency (EE%), % drug released after 12 h (Q12h), and particle size (PS). In vitro characterization, ex vivo intestinal permeation test, and pharmacokinetic study of the optimized formula were performed. A newly developed RP-HPLC technique was adopted for the estimation of EGCG. The optimized formula (F4) demonstrated more prolonged drug release and a significant improvement in the EE%, permeability, deformability and stability than the corresponding niosomes. The pharmacokinetic study investigated that F4 had a more sustained drug release and a higher bioavailability than the conventional niosomes and free drugs. Nanospanlastics could be a promising approach for improving the bioavailability of EGCG.

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DEVELOPMENT AND OPTIMIZATION OF MANNOSYLATED NARINGENIN LOADED TRANSFERSOMES USING RESPONSE SURFACE METHODOLOGY FOR SKIN CARCINOMA

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2021v13i2.40436 ◽

2021 ◽

pp. 235-241

Author(s):

NIKITA VERMA ◽

SWARNLATA SARAF

Keyword(s):

Free Radical ◽

Zeta Potential ◽

Ex Vivo ◽

Skin Permeation ◽

Research Work ◽

Radical Scavenging ◽

Entrapment Efficiency ◽

Mannose Receptor ◽

Skin Carcinoma

Objective: The flavonoidal drug Naringenin offers a natural defense against free radical generation due to their antioxidant i.e. free radical scavenging property. The continuation of research work towards the invention of targeting the flavonoidal drug for skin carcinoma. Naringenin is a potent antioxidant, having remarkable reactive oxygen species scavenging potential and abundantly found in citrus fruits. Methods: The optimization of the formulated mannosylated naringenin-loaded transfersomes (MA-NgTfs) was performed using Box–Behnken statistical design to obtain crucial variable parameters that influence vesicular size, size distribution and surface charge. Therefore keeping both the concepts in mind our objective is to design and optimize the mannosylated naringenin loaded transfersomes (MA-NgTfs) for macropahge targeting. The Box Behnken with 3D surface response design graph was employed to optimize the formulation. Results: Phospholipids and surfactant ratio played a remarkable role to determine the mean vesicular size and the Zeta potential of the vesicles. The Zeta potential is found in the formulation having a range of-18.01±1.05 to-28.7±1.008 mV represents the good stability of the formulation. The vesicles size range was found in the range of 102.4±1.01 to 263.74±0.63 and range of Entrapment efficiency of nanovesicles was as 72.04±1.53 to 82.04±0.81. In vitro drug release study shows that mannosylated naringenin loaded transfersomes (MA-NgTfs), and marketed formulation dispersion was found 69.31 %, 62.03 %, 58.71 %, and 65.02 % respectively. Ex vivo skin permeation and deposition study shows that the marketed product and pure drug suspension optimized transfersomes through the skin of mice was of flux 6.5±3.07 and the percentage of drug retention was 0.76±1.26. The results gave us strong evidence of cellular uptake bymannose–directed transfersomes via mannose receptor-based endocytosis. Conclusion: On the basis of findings, the study revealed that the prepared formulation has characteristic potential for targeting and the concept of ligand directed nanocarrier formulation was imparts synergistic effect against UV-induced skin carcinoma.

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FORMULATION AND EVALUATION OF MUCOADHESIVE MICROSPHERES OF AN ANTI-MIGRAINE DRUG

Journal of Drug Delivery and Therapeutics ◽

10.22270/jddt.v8i5.1943 ◽

2018 ◽

Vol 8 (5) ◽

pp. 465-474

Author(s):

S PADMA PRIYA ◽

AN Rajalakshmi ◽

P Ilaveni

Keyword(s):

Drug Release ◽

Sustained Release ◽

Sodium Alginate ◽

Release Kinetics ◽

Drug Loading ◽

Research Work ◽

Entrapment Efficiency ◽

Polyvinyl Pyrrolidone ◽

Anti Migraine Drug

Objective: The objective of this research work is to develop and evaluate mucoadhesive microspheres of an anti-migraine drug for sustained release. Materials and Methods: Mucoadhesive microspheres were prepared by emulsification method using Sodium alginate (SA), polyvinyl pyrrolidone (PVP) and Chitosan in the various drug-polymer ratios of 1:1, 1:2 and 1:3. Nine formulations were formulated and evaluated for possible drug polymer interactions, percentage yield, micromeritic properties, particle size, drug content, drug entrapment efficiency, drug loading, swelling index, In-vitro wash off test, in vitro drug release, surface morphology and release kinetics. Results: The results showed that no significant drug polymer interaction in FTIR studies. Among all the formulations SF3 containing sodium alginate showed 77.18% drug release in 6hrs. Conclusion: Amongst the developed mucoadhesive microspheres, SF3 formulation containing sodium alginate exhibited slow and sustained release in a controlled manner and it is a promising formulation for sustained release of Sumatriptan succinate. Keywords: Mucoadhesive microspheres, Sodium alginate, polyvinyl pyrrolidone, Chitosan, sustained release.

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DEVELOPMENT AND EVALUATION OF NANOPARTICULATE BASED IN-SITU GELLING SYSTEM FOR NASAL DRUG DELIVERY OF AN ANTI-EPILEPTIC DRUG

INDIAN DRUGS ◽

10.53879/id.54.09.10774 ◽

2017 ◽

Vol 54 (09) ◽

pp. 83-85

Author(s):

A Ambavkar ◽

◽

N. Desai

Keyword(s):

Drug Release ◽

Ex Vivo ◽

Entrapment Efficiency ◽

Poloxamer 407 ◽

Nasal Drug Delivery ◽

Anti Epileptic Drug ◽

Nanolipid Carriers ◽

In Situ Nasal Gel

The objective of the study was to develop and evaluate nanolipid carriers based in situ gel of Carbamazepine, for brain delivery through intranasal route. The non – invasive nasal route can provide rapid delivery of drugs directly to the central nervous system by bypassing the blood brain barrier. The nanolipid carriers of carbamazepine as in situ nasal gel can prolong the drug release for control of repetitive seizures and were prepared by Phase Inversion Temperature technique. The retention of the carriers in the nasal cavity was improved by using Poloxamer 407 as thermoresponsive and Carbopol 974P as mucoadhesive gelling polymers, respectively. The developed gel was evaluated for particle size, polydispersity index, zeta potential, morphology, entrapment efficiency, mucoadhesive and thermoresponsive behaviour, in vitro drug release, ex vivo permeation and nasociliotoxicity. The gel showed sustained release over prolonged periods and was found to be non-toxic to the sheep nasal mucosa.

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Investigating the potential of Quercetin enthused nano lipoidal system for the management of dermatitis

Research Journal of Pharmacy and Technology ◽

10.52711/0974-360x.2021.01127 ◽

2021 ◽

pp. 6516-6526

Author(s):

Deepti Dwivedi ◽

Shubham Pandey ◽

Shafaque Asif ◽

Vineet Awasthi ◽

Gurjeet Kaur ◽

...

Keyword(s):

Zeta Potential ◽

Skin Permeation ◽

Research Work ◽

Entrapment Efficiency ◽

Laser Scanning Microscopy ◽

Polydispersity Index ◽

In Vivo Studies ◽

Confocal Laser ◽

Skin Retention

Objective: The present research work was undertaken to develop quercetin enthused nanolipoidal systems and its characterization. The objective was to investigate potential of prepared system in the management of DNCB induced dermatitis. Method: Nanolipoidal system was prepared in different combinations with quercetin, L-α phosphatidylcholine (SPC) and ethanol and characterized for particle size, polydispersity index (PDI), zeta potential, drug entrapment efficiency, percentage drug release, skin retention and skin permeation. Selected batches were further incorporated into Carbopol 934 base gel. The vesicles were in size range 324.19-359 nm while polydispersity index (PDI) ranges from 0.241-0.554 and for zeta potential, it was from -26.33 to -39.3 nm. Entrapment efficiency was from 23.77-94.68 %. Confocal laser scanning microscopy showed penetration depth of rhodamine enthused ethosome across rat skin up to 45.23 µm which was significantly higher than the rhodamine solution (10 µm). In dinitrochlorobenzene (DNCB) induced mice dermatitis model histopathology study showed a marked decrease in amount of inflammatory cell nucleus in mice treated with quercetin loaded ethosomal gel followed by 76.13% decrease in-ear swelling and ear mass respectively in morphology study. The conventional marketed formulation showed a nominal decrease in epidermal thickness. Further Primary irritation index was less than 0.4 indicating negligible irritation in all the groups. Results: The optimized formulation F6 with SPC and ethanol in the ratio of 20:80 displayed the highest drug content and entrapment efficiency of 94.68±1.14%. PDI was 0.241±0.11 and skin retention 7.7%. Batch F6 with vesicle size and zeta potential of 324.9±19 nm and -26.33 mV, respectively, was incorporated in Carbopol 934 base gel and the prepared gel was evaluated for morphology, spreadability, in vitro, ex vivo release study, and kinetics study and in vivo studies. Conclusion: The present study revealed that the developed ethosomal gel can be used for enhanced delivery of Quercetin via skin. The in vitro studies indicated that the gel serves as an efficient carrier for Quercetin. It showed its effectiveness in the management of dermatitis. Further, Quercetin loaded nanoethosomal gel formulation can be viewed as a promising drug delivery system for the management of dermatitis.

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Development and In-Vitro Evaluation of pH Responsive Polymeric Nano Hydrogel Carrier System for Gastro-Protective Delivery of Naproxen Sodium

Advances in Polymer Technology ◽

10.1155/2019/6090965 ◽

2019 ◽

Vol 2019 ◽

pp. 1-13

Author(s):

Rai Muhammad Sarfraz ◽

Muhammad Rouf Akram ◽

Muhammad Rizwan Ali ◽

Asif Mahmood ◽

Muhammad Usman Khan ◽

...

Keyword(s):

Drug Release ◽

Naproxen Sodium ◽

Research Work ◽

Entrapment Efficiency ◽

Gravimetric Analysis ◽

X Ray Diffraction ◽

Scanning Calorimetry ◽

Swelling Behaviour ◽

X Ray

Current research work was carried out for gastro-protective delivery of naproxen sodium. Polyethylene glycol-g-poly (methacrylic acid) nanogels was developed through free radical polymerization technique. Formulation was characterized for swelling behaviour, entrapment efficiency, Fourier transform infrared (FTIR) spectroscopy, Differential scanning calorimetry (DSC), and Thermal Gravimetric Analysis (TGA), Powder X-ray diffraction (PXRD), Zeta size distribution, and Zeta potential measurements, and in-vitro drug release. pH dependent swelling was observed with maximum drug release at higher pH. PXRD studies confirmed the conversion of loaded drug from crystalline to amorphous form while Zeta size measurement showed size reduction. On the basis of these results it was concluded that prepared nanogels proved an effective tool for gastro-protective delivery of naproxen sodium.

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Topical Delivery of Meloxicam using Liposome and Microemulsion Formulation Approaches

Pharmaceutics ◽

10.3390/pharmaceutics12030282 ◽

2020 ◽

Vol 12 (3) ◽

pp. 282 ◽

Cited By ~ 4

Author(s):

Julia Zhang ◽

Anna Froelich ◽

Bozena Michniak-Kohn

Keyword(s):

Transdermal Delivery ◽

Oral Delivery ◽

Ex Vivo ◽

Skin Permeation ◽

Entrapment Efficiency ◽

Topical Delivery ◽

Onset Of Action ◽

Promising Alternative ◽

Inflammatory Drugs ◽

Systemic Onset

The aim of this study is to develop, characterize and compare conventional liposome, deformable liposome (transfersome) and microemulsion formulations as potential topical delivery systems for meloxicam. Liposomes were characterized in terms of vesicle size, zeta potential and entrapment efficiency. For microemulsions, particle size, electrical conductivity and viscosity studies were performed to assess the structure of the investigated systems. An ex vivo skin permeation study has been conducted to compare these formulations. The dermal and transdermal delivery of meloxicam using these formulations can be a promising alternative to conventional oral delivery of non-steroidal anti-inflammatory drugs (NSAIDs) with enhanced local and systemic onset of action and reduced side effects.

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Comparison of Rheological, Drug Release, and Mucoadhesive Characteristics upon Storage between Hydrogels with Unmodified or Beta-Glycerophosphate-Crosslinked Chitosan

International Journal of Polymer Science ◽

10.1155/2018/3592843 ◽

2018 ◽

Vol 2018 ◽

pp. 1-12 ◽

Cited By ~ 1

Author(s):

Emilia Szymańska ◽

Anna Czajkowska-Kośnik ◽

Katarzyna Winnicka

Keyword(s):

Drug Release ◽

Ex Vivo ◽

Physicochemical Characteristics ◽

Vaginal Mucosa ◽

Drug Release Profile ◽

Modified Chitosan ◽

Long Term Storage ◽

Crosslinked Chitosan ◽

Chitosan Hydrogels ◽

The Impact

The physicochemical characteristics of beta-glycerophosphate-crosslinked chitosan hydrogels were investigated upon long-term storage at ambient, accelerated, and refrigerated conditions and compared to unmodified chitosan formulations. Additionally, the impact of chitosan modification on the ex vivo mucoadhesive performance in contact with porcine vaginal mucosa and on the drug release profile from hydrogels was evaluated. Viscosity and mechanical properties of formulations with unmodified chitosan decreased significantly upon storage regardless of tested conditions as a result of hydrolytic depolymerization. Introduction of ion crosslinker exerted stabilizing effect on physicochemical performance of chitosan hydrogels but only upon storage at refrigerated conditions. Beta-glycerophosphate-modified chitosan formulations preserved organoleptic, rheological behavior, and hydrogel structure up to 3-month storage at 4 ± 2°C. Viscosity variations upon storage influenced markedly mucoadhesive properties and drug release rate from hydrogels.

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