FORMULATION AND OPTIMIZATION OF TOPICAL NANOEMULSION BASED GEL OF MOMETASONE FUROATE USING 32 FULL FACTORIAL DESIGN

INDIAN DRUGS ◽  
2021 ◽  
Vol 58 (06) ◽  
pp. 19-29
Author(s):  
Bhupendra G. Prajapati ◽  
◽  
Malay Jivani ◽  
Himanshu Paliwal ◽  
Keyword(s):  
Ex Vivo ◽  
Skin Permeation ◽  
In Vitro Release ◽  
Tween 80 ◽  
Stability Study ◽  
Mometasone Furoate ◽  
Gelling Agent ◽  
Topical Formulation ◽  
Topical Gel

Mometasone furoate (MF) is a glucocorticoid prodrug that faces the problem of poor aqueous solubility. Nanoemulsion-based topical gel of MF was formulated to enhance its solubility and potential of treating skin conditions. The selection of oil, surfactant and co-surfactant was done based on their solubility with the drug. The nanoemulsion was prepared using rose oil as the oil phase. Tween 80 and Transcutol P were used as surfactant and co-surfactant and they were blended in different ratios (1:0, 1:1, 2:1 and 3:1 w/w). The pseudo ternary diagrams were developed using these excipients and formulations exhibiting considerable nanoemulsion region were selected. The formulations were optimized by using Design Expert software for the globule size and cumulative percent release. The nanoemulsion formulations were characterized for in vitro release and stability study. The optimized nanoemulsions consisting of 2 % w/w oil, 30 % w/w Smix (Surfactant: Co-surfactant) and 67.9 % w/w water were consolidated into Carbopol 940 gelling agent to prepare three nanoemulsion-based gel formulations or nanoemulgels (NEG1-NEG3). Nanoemulgels were evaluated for their stability and ex vivo permeation of MF. The outcomes suggested that skin permeation of MF from all the nanoemulgel formulations was significantly enhanced as compared to the marketed mometasone furoate topical formulation.

Ultra-deformable Liposomes as Flexible Nanovesicular Carrier to Penetrate Versatile Drugs Transdermally

2020 ◽  
Vol 10 (1) ◽  
pp. 12-20
Author(s):  
Gaurav Tiwari ◽  
Ruchi Tiwari ◽  
Rachna Singh ◽  
Awani K. Rai
Keyword(s):  
Skin Permeation ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Stability Study ◽  
Human Organ ◽  
Ethanol Injection ◽  
Release Studies ◽  
Junction Protein ◽  
Penetration Ability

Introduction: Transferosomes also known as ultra-deformable liposomes were introduced by Gregor Cevc in 1990. These are deformable vesicles that transport drug across the skin, which is the best route of drug delivery because skin is the largest human organ with 3 kg total weight and a surface area of 1.5-2.0 m2. Methods: Transferosomes are able to efficiently deliver low as well as high molecular weight drug across the skin in terms of quantity and depth. Various methods used for the preparation of transferosomes such as thin film hydration method, reverse phase evaporation method, vortex/sonication method, ethanol injection method and freeze thaw method. Results: The prepared transferosomal preparation will be evaluated for particle shape and size, entrapment efficiency, stability study, penetration ability and skin permeation study. In vitro release studies are to be performed using a specific dissolution medium. Conclusion: Ultra deformable liposomes can be used for delivery of different drugs e.g. analgesic, anesthetic, corticosteroids, anticancer, sex hormone, insulin, gap junction protein, and albumin.

scholarly journals Development of a Topical Amphotericin B and Bursera graveolens Essential Oil-Loaded Gel for the Treatment of Dermal Candidiasis

2021 ◽  
Vol 14 (10) ◽  
pp. 1033
Author(s):  
Lupe Carolina Espinoza ◽  
Lilian Sosa ◽  
Paulo C. Granda ◽  
Nuria Bozal ◽  
Natalia Díaz-Garrido ◽  
...  
Keyword(s):  
Essential Oil ◽  
Amphotericin B ◽  
Ex Vivo ◽  
In Vitro Release ◽  
Topical Administration ◽  
In Vivo Models ◽  
Topical Gel ◽  
Cutaneous Candidiasis ◽  
Vitro Release

The higher molecular weight and low solubility of amphotericin B (AmB) hinders its topical administration. The aim of this study was to incorporate Bursera graveolens essential oil into an AmB topical gel (AmB + BGEO gel) in order to promote the diffusion of the drug through the skin in the treatment of cutaneous candidiasis. AmB + BGEO gel formulation was determined using a factorial experiment. Physical and chemical parameters, stability, in vitro release profile and ex vivo permeation in human skin were evaluated. In vitro antimicrobial activity was studied using strains of C. albicans, C. glabrata and C. parapsilosis. The tolerability was evaluated using in vitro and in vivo models. AmB + BGEO gel presented appropriate characteristics for topical administration, including pH of 5.85, pseudoplastic behavior, optimal extensibility, as well as high stability and acceptable tolerability. In vitro release studies showed that the formulation releases the drug following a Boltzmann sigmoidal model. Finally, AmB + BGEO gel exhibited higher amount of drug retained inside the skin and lower Minimum Inhibitory Concentration than a formulation sans essential oil. Therefore, these results suggest that the incorporation of B. graveolens essential oil in the formulation could be used as strategy to promote a local effect in the treatment of cutaneous candidiasis.

scholarly journals ENHANCING THE SUNSCREEN EFFICACY OF BEMOTRIZINOL MICROPIGMENT BY USING O/W NANOEMULSION TOPICAL PREPARATIONS

2019 ◽  
pp. 47-56
Author(s):  
Dina Medhat Hashim ◽  
Nermin Mohamed Sheta ◽  
Vivian Samir Elwazzan ◽  
Wedad Saed Sakran
Keyword(s):  
Ex Vivo ◽  
In Vitro Release ◽  
Tween 80 ◽  
Size Analysis ◽  
Isopropyl Myristate ◽  
Tape Stripping ◽  
Protection Factor ◽  
Potential Measurement ◽  
Optimum Formula

Objective: Bemotrizinol (BEMT) is the most efficient broad-spectrum UV-absorber having a dual mechanism of action in absorbing and reflecting photons. The main objective of this work was to develop successful oil in water (o/w) nanoemulsion for improving the solubility of BEMT and its protective characteristics. Methods: Pseudo-ternary phase diagrams were constructed using labrafac PG and isopropyl myristate as oil phase, tween 80 as surfactant (S) and cremophor EL as cosurfactant (CoS) the ratio of S/CoS was determined according to highest percent of water incorporation to the system. Full factorial study design (24) using Design-Expert® software was adopted to study the effect of four independent variables namely: oil type, oil concentration, S/CoSmix (3:1) concentrations and BEMT concentration on the particle size and the in vitro release at 2 h (Q2h) of the prepared nanoemulsion formulae. Two systems each of eight formulae were developed and evaluated through droplet size analysis, zeta potential measurement, refractive index, in vitro drug release and according to the desirability value two formulae (F6 and F14) were used for further evaluations including in vitro sun protection factor (SPF), ex-vivo deposition by tape stripping technique, permeation test and photostability study. Results: Formula (F14) was chosen as the optimum formula having an in vitro SPF of 16.08±0.39, lowest permeation of 140±0.06 μg/cm2after six h and highest photostability (t90% = 168.02) after 120 min. Conclusion: Despite the poor solubility of bemotrizinol, it could be enhanced by novel drug delivery systems with good SPF value while maintaining its photostability.

Design and Development of Clobetasol Propionate Topical Gel Thickened with Novel Copolymer

2017 ◽  
Vol 7 (04) ◽  
Author(s):  
Kumar Pawan ◽  
Shailendra Kumar Singh
Keyword(s):  
Drug Release ◽  
Water Solubility ◽  
In Vitro Release ◽  
Gelling Agent ◽  
In Vitro Drug Release ◽  
Promising Alternative ◽  
Topical Gel ◽  
Release Studies ◽  
Photo Stability

Topical delivery of clobetasole propionate (CP) offers several formulation related problems due to poor water solubility and photo degradation property. In the present investigation, topical gel of CP was formulated using Acrylamide/ Sodium Acryloyldimethyl taurate copolymer (SEPINEO™ P 600) as a gelling agent and evaluated with respect to different physicochemical parameters such as pH, viscosity, bio-adhesivity, spreadability, in vitro drug release and photo stability. Permeation of CP gel was studied using freshly excised pig ear skin for 24 h. The cumulative permeation of drug through excised rat skin was 3.0 ± 1.2 mg cm-2 with the corresponding flux value of 0.24 ± 0.09 mg cm-2 h -1 . The in vitro release studies showed 101.43±1.12 % drug release over 10 h. The selected formulation was found to be effective with respect to percent drug content, permeation characteristics, pH, viscosity, and photostability. Therefore, CP gel could be very promising alternative for the topical drug delivery.

Studies with Emulsion Containing trans-resveratrol: in vitro Release Profile and ex vivo Human Skin Permeation

2015 ◽  
Vol 12 (2) ◽  
pp. 157-165 ◽  
Author(s):  
Priscila de Almeida ◽  
Michele Alves ◽  
Hudson Polonini ◽  
Stephane Calixto ◽  
Tiago Braga Gomes ◽  
...  
Keyword(s):  
Human Skin ◽  
Ex Vivo ◽  
Skin Permeation ◽  
In Vitro Release ◽  
Release Profile ◽  
Vitro Release

Acitretin loaded Nanocarrier gel: formulation and exploration of in-vitro release kinetics

2021 ◽  
Vol 11 ◽  
Author(s):  
Anupriya Kapoor ◽  
Nikunj sethi ◽  
Navneet Verma
Keyword(s):  
Patient Compliance ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Oral Route ◽  
The Body ◽  
Gelling Agent ◽  
Ionic Surfactant ◽  
Topical Formulation ◽  
Vitro Release

Background: Psoriasis is an autoimmune disorder that affects the skin and is characterized by irritation, red, flaky patches over different parts of the body. The present study intended to design and evaluate Acitretin (ACT) loaded nanostructured lipid carriers (NLCs) to manage psoriasis through topical application. ACT is an analog of vitamin A used to control psoriasis via the oral route. The prime demerit associated with oral route delivery of a drug is the teratogenic effect associated with the active molecule and side effects like dry mouth, runny nose, hair loss, taste changes, chapped lips, etc. These are the major contributing factors to reduced patient compliance. Objective: The objective of the present research work was to develop a topical formulation of ACT. Developing topical formulation for the same can result in enhanced patient compliance and can be worth compared to the marketed oral formulation of the drug. Methods: ACT loaded NLCs were prepared by hot homogenization method using oleic acid as a liquid lipid and stearic acid as a solid lipid in a 7:3 ratio along with the combination of a non-ionic surfactant (Tween 80) and an anionic surfactant ( sodium lauryl sulphate). Results: In several optimization experiments formulation, F3 was found to be most appropriate for formulating gel. Morphological information obtained from SEM reinforced the formation of particles with nearly spherical morphology. The optimized formulation had a mean diameter of 363nm, as founded by Zetasizer. XRD studies affirmed that the formulation exhibits amorphous nature, which is an essential character of NLC. An optimized formulation was further incorporated in the gel by using Carbopol 940P as a gelling agent. In vitro release studies indicated 96.85 ± 2% release in 8 hours with Korsmeyer- Peppas model release kinetics. The observed n value1.391 for drug release for F3G2 bespeak Super case II transport maybe result from sorption of the drug from the surface of NLC controlled by stress-induced relaxation boundary of the swollen shell. Conclusion: In vitro characterization of ACT (Acitretin) loaded NLC supports the objective that NLC can serve as a potential carrier for topical delivery of ACT and can also reduce oral toxicity associated with drug after stringent evaluation in the near future.

scholarly journals Evaluation of Skin Permeation and Analgesic Activity Effects of Carbopol Lornoxicam Topical Gels Containing Penetration Enhancer

2014 ◽  
Vol 2014 ◽  
pp. 1-9 ◽  
Author(s):  
Saleh A. Al-Suwayeh ◽  
Ehab I. Taha ◽  
Fahad M. Al-Qahtani ◽  
Mahrous O. Ahmed ◽  
Mohamed M. Badran
Keyword(s):  
Analgesic Activity ◽  
Skin Permeation ◽  
Tween 80 ◽  
Skin Penetration ◽  
Penetration Enhancers ◽  
Topical Gel ◽  
Carbopol Gel ◽  
Franz Diffusion Cells ◽  
Gel Formulations

The current study was designed to develop a topical gel formulation for improved skin penetration of lornoxicam (LOR) for enhancement of its analgesic activity. Moreover, the effect of different penetration enhancers on LOR was studied. The LOR gel formulations were prepared by using hydroxylpropyl methylcellulose (HPMC) and carbopol. The carbopol gels in presence of propylene glycol (PG) and ethanol were developed. The formulated gels were characterized for pH, viscosity, and LOR release using Franz diffusion cells. Also,in vitroskin permeation of LOR was conducted. The effect of hydroxypropylβ-cyclodextrin (HPβ-CD), beta-cyclodextrin (β-CD), Tween 80, and oleic acid on LOR permeation was evaluated. The optimized LOR gel formulation (LORF8) showed the highest flux (14.31 μg/cm2/h) with ER of 18.34 when compared to LORF3. Incorporation of PG and HPβ-CD in gel formulation (LORF8) enhanced the permeation of LOR significantly. It was observed that LORF3 and LORF8 show similar analgesic activity compared to marketed LOR injection (Xefo). This work shows that LOR can be formulated into carbopol gel in presence of PG and HPβ-CD and may be promising in enhancing permeation.

scholarly journals USE OF CASHEW BARK EXUDATE GUM IN THE PREPARATION OF 4 % LIDOCAINE HCL TOPICAL GELS

2017 ◽  
Vol 9 (8) ◽  
pp. 146 ◽  
Author(s):  
M. Saquib Hasnain ◽  
Poonam Rishishwar ◽  
Sadath Ali
Keyword(s):  
Ex Vivo ◽  
Skin Permeation ◽  
Stability Study ◽  
Current Work ◽  
Topical Gel ◽  
Thaw Cycle ◽  
Ex Vivo Permeation ◽  
Freeze Thaw Cycle ◽  
Lidocaine Hcl ◽  
Topical Gels

Objective: The objective of the current work was to prepare and evaluate ex vivo skin permeation of cashew bark exudate gum based 4 % lidocaine HCl topical gels.Methods: In the current work, 4 % lidocaine HCl topical gels were prepared by using different concentrations of cashew bark exudate gum, HPMC K4M, lidocaine HCl, methyl paraben (as preservative) and glycerin (as plasticizer). The formulated topical gels were evaluated for pH, viscosity, and ex vivo skin permeation through excised porcine ear skin membrane.Results: The pHs of these formulated 4 % lidocaine HCl topical gels were found within the range of 6.04±0.02 to 6.52±0.04; whereas, the viscosities were measured within the range, 4.38±0.02 x 106to 4.74±0.04 x 106 cps. Sustained ex vivo permeation of lidocaine was measured over 7 h. Highest ex vivo permeation flux was measured when 0.1 % menthol was incorporated as a permeation enhancer. It was also higher than that of the marketed 4 % lidocaine HCl topical gel. The stability study by freeze thaw cycle method revealed physically stable gels without the occurrence of syneresis.Conclusion: The results clearly indicate a promising potential of the use of cashew bark exudate gum as a gelling material with HPMC K4M to prepare 4 % lidocaine HCl topical gels of good skin permeation capability

scholarly journals Enhancement of Curcumin Anti-Inflammatory Effect via Formulation into Myrrh Oil-Based Nanoemulgel

Polymers ◽  
2021 ◽  
Vol 13 (4) ◽  
pp. 577 ◽  
Author(s):  
Wafaa E. Soliman ◽  
Tamer M. Shehata ◽  
Maged E. Mohamed ◽  
Nancy S. Younis ◽  
Heba S. Elsewedy
Keyword(s):  
Ex Vivo ◽  
Skin Permeation ◽  
In Vitro Release ◽  
Aqueous Solubility ◽  
Delivery Methods ◽  
Anti Cancer ◽  
Permeation Studies ◽  
Anti Inflammatory

Background: Curcumin (Cur) possesses a variety of beneficial pharmacological properties including antioxidant, antimicrobial, anti-cancer and anti-inflammatory activities. Nevertheless, the low aqueous solubility and subsequent poor bioavailability greatly limits its effectiveness. Besides, the role of myrrh oil as an essential oil in treating inflammatory disorders has been recently demonstrated. The objective of the current investigation is to enhance Cur efficacy via developing Cur nanoemulgel, which helps to improve its solubility and permeability, for transdermal delivery. Methods: The formulated preparations (Cur gel, emulgel and nanoemulgel) were evaluated for their physical appearance, spreadability, viscosity, particle size, in vitro release and ex vivo drug permeation studies. The in vivo anti-inflammatory activity was estimated using the carrageenan-induced rat hind paw edema method. Results: The formulated Cur-loaded preparations exhibited good physical characteristics that were in the acceptable range of transdermal preparations. The release of Cur from gel, emulgel and nanoemulgel after 12 h was 72.17 ± 3.76, 51.93 ± 3.81 and 62.0 ± 3.9%, respectively. Skin permeation of Cur was significantly (p < 0.05) improved when formulated into nanoemulgel since it showed the best steady state transdermal flux (SSTF) value (108.6 ± 3.8 µg/cm2·h) with the highest enhancement ratio (ER) (7.1 ± 0.2). In vivo anti-inflammatory studies proved that Cur-loaded nanoemulgel displayed the lowest percent of swelling (26.6% after 12 h). Conclusions: The obtained data confirmed the potential of the nanoemulgel dosage form and established the synergism of myrrh oil and Cur as an advanced anti-inflammatory drug.

scholarly journals Vegetable Oil-Based Self-Microemulsifying Drug Delivery System of Eprosartan Mesylate: in vitro and ex vivo Evaluation

2021 ◽  
Vol 33 (9) ◽  
pp. 2182-2190
Author(s):  
Sabitri Bindhani ◽  
Snehamayee Mohapatra ◽  
Rajat Kumar Kar
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Delivery System ◽  
Intestinal Permeability ◽  
Delivery System ◽  
Ex Vivo ◽  
Tween 80 ◽  
Stability Study ◽  
Potent Drug

This study was planned to increase the intestinal permeability and thereby bioavailability of eprosartan mesylate (EPM) by designing a self-microemulsifying drug delivery system (SMEDDS) by the use of vegetable oils. Various SMEDDS-based formulations were prepared with oleic acid and peppermint oil. Tween 80 was used as surfactant and PEG 400 as co-surfactant. Pseudo ternary phase diagrams were constructed for identifying emulsification region between 1:1, 1:2, 2:1, 3:1 ratio of SCOS mix. Eight batches of SMEDDS were found to be thermodynamically stable and from which SMEDDSOF9 and PF5 were best formulations due to their highest drug content, minimum particle size. They have shown highest release of drug in vitro and higher in vitro drug diffusion and ex vivo permeation analysis than pure drug. FTIR study ascertained no incompatibility between drug and excipients present in formulation. From the accelerated stability study, slight effect on particle size and zeta potential, assay content along with cumulative % of drug release was found. The results demonstrated the SMEDDS of EPM are potent drug delivery system to increase dissolution rate and bioavailability of drug via increased intestinal permeability and consequently improving the therapeutic efficacy of eprosartan mesylate.

Sign in / Sign up

Export Citation Format

Share Document