scholarly journals Gamma oryzanol niosomal gel for skin cancer: formulation and optimization using quality by design (QbD) approach

AAPS Open ◽  
2021 ◽  
Vol 7 (1) ◽  
Author(s):  
Harsh S. Shah ◽  
Ankit Gotecha ◽  
Dolly Jetha ◽  
Amarjitsing Rajput ◽  
Aditi Bariya ◽  
...  
Keyword(s):  
Skin Cancer ◽  
Quality By Design ◽  
Rice Bran Oil ◽  
Ex Vivo ◽  
Entrapment Efficiency ◽  
Molar Ratio ◽  
Ex Vivo Permeation ◽  
Permeation Studies ◽  
Niosomal Gel ◽  
Gamma Oryzanol

AbstractSkin cancer is fifth most diagnosed disease in human population due to ultraviolet radiation (UV) exposure. Gamma oryzanol (OZ) is a natural antioxidant, and it also has skin anti-aging properties. OZ is naturally found in rice bran oil. The main aim of the present work was to optimize OZ niosomal formulation using quality by design approach including one variable at a time and full factorial design. Niosomes were prepared by solvent injection method and characterized for size, polydispersity index, drug entrapment, and transmission electron microscopy. The optimized batch obtained at X1 [drug to span 60 molar ratio (1:5)], X2 [volume of hydration (75 mL)], and X3 [stirring speed (2500 rpm)] to Y1 [average vesicle size (196.6 nm)] and Y2 [entrapment efficiency (78.31%)] as dependent variables. The optimized OZ noisomes were formulated by niosomal gel to provide improved physicochemical stability upon topical application against UV. The niosomal gel was characterized using pH meter, viscometer, Draize test for skin irritancy, ex vivo permeation studies, and stability studies. Ex vivo permeation studies of OZ niosomal gel not only showed fourfold higher permeation but also exhibited better drug retention in dermal layers of skin as compared to OZ gel. Quality Target Product Profile of OZ niosomal formulation was generated. Risk analysis of optimized OZ gel suggested most critical quality attributes (CQAs) and critical process parameters (CPPs) to be characterized as low risk. Thus, γ-oryzanol niosomal gel for topical use can serve as a promising prophylactic treatment in skin cancer, and the developed prototype formulation can be further extended to future newly discovered drugs with similar characteristics. Graphical abstract

Development and Characterization of Apremilast Transethosomal Gel for Transdermal Delivery

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.

scholarly journals Serratiopeptidase Niosomal Gel with Potential in Topical Delivery

2014 ◽  
Vol 2014 ◽  
pp. 1-9 ◽  
Author(s):  
Ujwala A. Shinde ◽  
Shivkumar S. Kanojiya
Keyword(s):  
Ex Vivo ◽  
Skin Permeation ◽  
Entrapment Efficiency ◽  
Molar Ratio ◽  
Fourfold Increase ◽  
Surfactant Vesicles ◽  
Anti Inflammatory ◽  
Niosomal Gel

The objective of present study was to develop nonionic surfactant vesicles of proteolytic enzyme serratiopeptidase (SRP) by adapting reverse phase evaporation (REV) technique and to evaluate the viability of SRP niosomal gel in treating the topical inflammation. The feasibility of SRP niosomes by REV method using Span 40 and cholesterol has been successfully demonstrated in this investigation. The entrapment efficiency was found to be influenced by the molar ratio of Span 40 : cholesterol and concentration of SRP in noisome. The developed niosomes were characterized for morphology, particle size, and in vitro release. Niosomal gel was prepared by dispersing xanthan gum into optimized batch of SRP niosomes. Ex vivo permeation and in vivo anti-inflammatory efficacy of gel formulation were evaluated topically. SRP niosomes obtained were round in nanosize range. At Span 40 : cholesterol molar ratio 1 : 1 entrapment efficiency was maximum, that is, 54.82% ± 2.08, and showed consistent release pattern. Furthermore ex vivo skin permeation revealed that there was fourfold increase in a steady state flux when SRP was formulated in niosomes and a significant increase in the permeation of SRP, from SRP niosomal gel containing permeation enhancer. In vivo efficacy studies indicated that SRP niosomal gel had a comparable topical anti-inflammatory activity to that of dicolfenac gel.

Proniosomes as Nano-Carrier for Transdermal Delivery of Atenolol Niosomal Gel

2017 ◽  
Vol 7 (04) ◽  
Author(s):  
El-Assal M I A
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Entrapment Efficiency ◽  
Cellulose Membrane ◽  
Order Kinetic ◽  
In Vitro Drug Release ◽  
Ex Vivo Permeation ◽  
Niosomal Gel ◽  
Optimum Formula

Objective of the study is to prepare Proniosomes that refers to a flexible vesicular carrier with the potential for drug administration through the transdermal route. Medthod: Proniosomes were prepared by the coacevation-phase separation technique The prepared formulations were evaluated for vesicle size, entrapment efficiency. The optimal poniosomes formula (A8) was prepared with different aqueous phase, incorporated in a gel base and studied for pH, viscosity, spredapility, stability, in vitro drug release and ex vivo permeation. Results: Niosomes formulations prepared with Span 40 and 60 have spherical and smaller Nano size. 25 mg atenolol loading has resulted 190.9 ± 15.033 nm sizes. EE% of the optimum formula prepared with distilled water was 62.11 to 92.38 .Rheological behavior showed combined shear thinning and thixotropic and gel was spreadable . Tested formulations were stable on cooling (4-8 oC) . In vitro drug release followed zero order kinetic, and gave sustained release. Release rate was significantly higher across cellulose membrane compared with rate skin. Amount of drug obtained after skin extraction was 92.6 ± 0.5% indicate enhanced permeation rate. Conclusion: All the proniosomal gel formulations were found through the acceptable range of vascular size and entrapment efficiency. Formulation A8 has been selected as an optimized therapeutic system of atenolol.

scholarly journals FORMULATION AND EVALUATION OF ACECLOFENAC PRONIOSOME LOADED ORABASE FOR MANAGEMENT OF DENTAL PAIN

2018 ◽  
Vol 10 (6) ◽  
pp. 204
Author(s):  
G. V. Radha ◽  
K Trideva Sastri ◽  
P. Prathyusha ◽  
P. Bhanu ◽  
Jampala Rajkumar
Keyword(s):  
Ex Vivo ◽  
Entrapment Efficiency ◽  
Prolonged Release ◽  
Particle Size Range ◽  
Sem Images ◽  
Ex Vivo Permeation ◽  
Main Motive ◽  
Permeation Studies ◽  
Span 60

Objective: The main motive is to develop proniosomes loaded orabase for enhanced permeation and prolonged release of aceclofenac for oro dental conditions.Methods: Various aceclofenac (ACL) proniosomal gels were formulated employing various surfactants, span 60 was superior and significant for loading into orabase. The formulations were scrutinized for entrapment efficiency, optical microscopy, in vitro diffusion and release studies, mucoadhesive strength, ex-vivo permeation studies and drug-excipient interactions were determined by FTIR spectroscopy.Results: Considering best entrapment efficiency with span 60 (97.60±1.85) and optimum vesicle shape, along with prolonged drug permeation (45% for 24 h) the formulation F(ACL)1 was selected and optimized for loading into orabase. The F(ACL)1 loaded orabase exhibited significant prolonged release over 14 h, and permeation profiles exhibited nearly two-fold increased flux in comparison with control. Good mucoadhesive strength was observed for proniosomal orabase 6370 dynes/cm2. No evidence of incompatibility amongst formulation components from FTIR studies. SEM images revealed the particle size range from 136 µm to 236 µm for proniosomal orabase.Conclusion: Orabase can be an effective carrier for proniosomes with enhanced permeation and prolonged release for oro-dental conditions.

STUDIES ON NANOLIPID EMULGEL OF NIMESULIDE FOR TRANSDERMAL DELIVERY

INDIAN DRUGS ◽  
2019 ◽  
Vol 56 (09) ◽  
pp. 74-77
Author(s):  
C Trimukhe ◽  
P. Patil ◽  
K. Sheth ◽  
N. Desai ◽  
Keyword(s):  
Ex Vivo ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Spherical Particles ◽  
Sustained Drug Release ◽  
Polyethylene Glycol 400 ◽  
Ex Vivo Permeation ◽  
Nanometric Range ◽  
Permeation Studies

The objective of the present study was to develop and evaluate a nanolipid transdermal emulgel of Nimesulide. The nanolipid particles of Nimesulide were developed using Compritol 888 ATO and Labrafil M1944 as lipids, Polysorbate 80 as surfactant with Poloxamer 188 and Polyethylene Glycol 400 as stabilizer and cosolvent respectively. The nanoparticles were developed by Hot Nanoemulsification Low Temperature Solidification method and showed drug entrapment efficiency of 67 ± 2.316 % with particle size of 500 – 600 nm. TEM studies indicated presence of spherical particles in the nanometric range. The nanolipidic dispersions were suitably gelled to form emulgel. The in vitro release of the developed emulgel showed sustained drug release for 8 hours with no evidence of toxicity during histopathological testing after ex vivo permeation studies. The nanolipid emulgel of Nimesulide can thus provide sustained release action due to enhanced skin deposition for effective treatment of chronic arthritic conditions, thereby improving patient compliance.

scholarly journals Formulation and Evaluation of Lignocaine Hydrochloride Proniosomes Loaded Orabase for Dental Anaesthesia

2021 ◽  
Vol 11 (3-S) ◽  
pp. 27-34
Author(s):  
Radha G. V. ◽  
GANESH SAI MYNENI ◽  
Sunayana N ◽  
Soujanya G. V. R. L. ◽  
Charan K
Keyword(s):  
Ex Vivo ◽  
Entrapment Efficiency ◽  
Prolonged Release ◽  
Particle Size Range ◽  
Sem Images ◽  
Ex Vivo Permeation ◽  
Vesicle Shape ◽  
Permeation Studies ◽  
Span 80

The aim of this research is to prepare and evaluate lignocaine HCl Proniosomal orabase for enhanced permeation and prolonged dental anaesthesia effect. Objective: Various lignocaine proniosomal gels were formulated employing various surfactants. Methods: The formulations were scrutinized for entrapment efficiency, optical microscopy, in-vitro diffusion and release studies, mucoadhesive strength, ex-vivo permeation studies and drug – excipient interactions were determined by FTIR spectroscopy. Results: span 80 was found to be superior and significant for loading in to orabase. Considering the best entrapment efficiency with span 80 (91.60%) and optimum vesicle shape, along with prolonged drug permeation (33.6% for 24 h) the formulation F4 was selected and optimized for loading into orabase. The formulation F4 loaded orabase exhibited significant prolonged release over 10 h, and permeation profiles exhibited nearly two – fold increased flux in comparison with control. Good mucoadhesive strength was observed for proniosomal orabase 6273dynes/cm2, No evidence of incompatibility amongst formulation components from FTIR studies. SEM images revealed the particle size range from 50 μmt to 100 μmt for proniosomal orabase. Conclusion: Orabase can be an effective carrier for proniosomes with enhanced retention time at the site of application and provide prolonged release for oro-dental conditions. Keywords: lignocaine Hcl, Oro-dental anaesthesia, Proniosomal gel, Orabase, Entrapment efficiency, prolonged release.

Development, Pre-clinical Investigation and Histopathological Evaluation of Metronidazole Loaded Topical Formulation for Treatment of Skin Inflammatory disorders

2020 ◽  
Vol 10 ◽  
Author(s):  
Divya Thakur ◽  
Gurpreet Kaur ◽  
Sheetu Wadhwa ◽  
Ashana Puri
Keyword(s):  
Ex Vivo ◽  
Clinical Investigation ◽  
In Vivo Studies ◽  
Tween 20 ◽  
Inflammatory Disorders ◽  
Rat Paw Edema ◽  
Ex Vivo Permeation ◽  
Permeation Studies ◽  
Anti Inflammatory

Background: Metronidazole (MTZ) is an anti-oxidant and anti-inflammatory agent with beneficial therapeutic properties. The hydrophilic nature of molecule limits its penetration across the skin. Existing commercial formulations have limitations of inadequate drug concentration present at target site, which requires frequent administration and poor patient compliance. Objective: The aim of current study was to develop and evaluate water in oil microemulsion of Metronidazole with higher skin retention for treatment of inflammatory skin disorders. Methods: Pseudo ternary phase diagrams were used in order to select the appropriate ratio of surfactant and co-surfactant and identify the microemulsion area. The selected formulation consisted of Capmul MCM as oil, Tween 20 and Span 20 as surfactant and co-surfactant, respectively, and water. The formulation was characterized and evaluated for stability, Ex vivo permeation studies and in vivo anti-inflammatory effect (carrageenan induced rat paw edema, air pouch model), anti-psoriatic activity (mouse-tail test). Results: The particle size analyses revealed average diameter and polydispersity index of selected formulation to be 16 nm and 0.373, respectively. The results of ex vivo permeation studies showed statistically higher mean cumulative amount of MTZ retained in rat skin from microemulsion i.e. 21.90 ± 1.92 μg/cm2 which was 6.65 times higher as compared to Marketed gel (Metrogyl gel®) with 3.29 ± 0.11 μg/cm2 (p<0.05). The results of in vivo studies suggested the microemulsion based formulation of MTZ to be similar in efficacy to Metrogyl gel®. Conclusion: Research suggests efficacy of the developed MTZ loaded microemulsion in treatment of chronic skin inflammatory disorders.

Transdermal delivery of naloxone: ex vivo permeation studies

1999 ◽  
Vol 179 (1) ◽  
pp. 129-134 ◽  
Author(s):  
Jagdish Jaiswal ◽  
Ramarao Poduri ◽  
Ramesh Panchagnula
Keyword(s):  
Transdermal Delivery ◽  
Ex Vivo ◽  
Ex Vivo Permeation ◽  
Permeation Studies

Photostability and ex-vivo permeation studies on diclofenac in topical niosomal formulations

2015 ◽  
Vol 494 (1) ◽  
pp. 490-497 ◽  
Author(s):  
Giuseppina Ioele ◽  
Lorena Tavano ◽  
Michele De Luca ◽  
Gaetano Ragno ◽  
Nevio Picci ◽  
...  
Keyword(s):  
Ex Vivo ◽  
Ex Vivo Permeation ◽  
Permeation Studies

scholarly journals Olive Oil Based Organogels for Effective Topical Delivery of Fluconazole: In-vitro Antifungal Study

2020 ◽  
pp. 29-36
Author(s):  
Mohammad Muqtader Ahmed ◽  
Farhat Fatima ◽  
Abdul Bari Mohammed
Keyword(s):  
Olive Oil ◽  
Ex Vivo ◽  
Similarity Index ◽  
Ex Vivo Permeation ◽  
Efficient Delivery ◽  
In Vitro Diffusion ◽  
Permeation Studies ◽  
The Stability ◽  
Hot Melt

The objective of the study was to formulate olive oil based organogels for the topical application of fluconazole (FLZ), to ensure the efficient delivery of the drug deeper in to the skin layers. Methods: Nine formulations developed by hot-melt method using olive oil, sorbitan monostearate (SMS) and FLZ. Prepared formulations characterized for macro evaluations, pH, spreadibility, viscosity, gel-sol transition, in-vitro diffusion study. Further optimized formulation evaluated for ex-vivo percutaneous permeation, in-vitro antifungal studies and stability studies by similarity index. Results: The results of evaluated parameters ensure the stability and effectiveness of the prepared olive oil based organogels. In-vitro diffusion studied reflects decrease in drug release with increase in surfactant concentration due to increase in viscosity. Moreover, ex-vivo permeation studies revealed that the permeation of FLZ was enhanced for optimized formulations (F6) as compared to the marketed gel formulation. Further, the optimized formulation exhibits the broad zone of inhibition against fungal strains in comparison to control and marketed product during in-vitro antifungal study. Conclusion: The olive oil based organogels formulation shown the enhanced permeation of FLZ from organogel network structure with good antifungal activity as compared to the marketed formulation. Henceforth, the FLZ organogel formulations could be used topically for the effective treatment of fungal infection.

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