scholarly journals Advanced development of a non-ionic surfactant and cholesterol material based niosomal gel formulation for the topical delivery of anti-acne drugs

2020 ◽  
Vol 1 (6) ◽  
pp. 1763-1774 ◽  
Author(s):  
Akhilesh Shah ◽  
Sanjay Boldhane ◽  
Atmaram Pawar ◽  
Chellampillai Bothiraja
Keyword(s):  
Therapeutic Efficacy ◽  
Topical Delivery ◽  
Ionic Surfactant ◽  
Topical Gel ◽  
Niosomal Gel ◽  
Advanced Development ◽  
Low Solubility

The aim of the present investigation was to develop adapalene (ADP), a high lipophilicity and low solubility anti-acne drug-loaded niosomal topical gel formulation, in order to improve its therapeutic efficacy.

Nanotechnological Innovations Enhancing the Topical Therapeutic Efficacy of Quercetin: A Succinct Review

2020 ◽  
Vol 17 (4) ◽  
pp. 270-278
Author(s):  
Maha Nasr ◽  
Rawan Al-Karaki
Keyword(s):  
Side Effects ◽  
Therapeutic Efficacy ◽  
Skin Permeation ◽  
Skin Penetration ◽  
Topical Delivery ◽  
Natural Compounds ◽  
Therapeutic Activity ◽  
Dermatological Diseases ◽  
Anti Inflammatory ◽  
Topical Applications

Nanotechnology is currently a hot topic in dermatology and nutraceutical/cosmeceutical delivery, owing to the advantages it provides in terms of enhancing the skin permeation of drugs, as well as increasing their therapeutic efficacy in the treatment of different dermatological diseases. There is also a great interest in the topical delivery of nutraceuticals; which are natural compounds with both therapeutic and cosmetic benefits, in order to overcome the side effects of topically applied chemical drugs. Quercetin is a key nutraceutical with topical antioxidant and anti-inflammatory properties which was reported to be effective in the treatment of different dermatological diseases, however, its topical therapeutic activity is hindered by its poor skin penetration. This review highlights the topical applications of quercetin, and summarizes the nanocarrier-based solutions to its percutaneous delivery challenges.

Development and Evaluation of Particulate Microcarriers of Adapalene as a Topical Delivery System

2019 ◽  
Vol 9 (3) ◽  
pp. 222-233
Author(s):  
Divya D. Jain ◽  
Namita D. Desai
Keyword(s):  
Patient Compliance ◽  
Targeted Delivery ◽  
Ex Vivo ◽  
Acne Vulgaris ◽  
Drug Loading ◽  
Topical Therapy ◽  
Skin Irritation ◽  
Topical Delivery ◽  
Diffusion Method ◽  
Topical Gel

Background: Adapalene is a promising third generation retinoid used in the topical treatment of acne vulgaris. However, the major drawback associated with conventional topical therapy of Adapalene is the ‘retinoid reaction’ which is dose-dependent and characterized by erythema, scaling and burning sensation at the application sites. Microparticulate drug delivery can play a major role in reducing side effects and providing better patient compliance due to targeted delivery. Methods: Adapalene microparticles were prepared using quasi emulsion solvent diffusion method. The effects of formulation variables including polymer ratios, amounts of emulsifier, drug loading and process variables such as stirring time and speed on the physical characteristics of microparticles were investigated. The developed microparticles were characterized by DSC and SEM. Adapalene microparticles were incorporated into Carbopol 971 NF gel for ease of topical delivery. Results: Adapalene microparticulate topical gel showed sustained drug release over 8 hours in in vitro studies. The amount of drug retained in the rat skin during ex vivo studies was higher in the microparticulate topical gel (227.43 ± 0.83 µg/cm2) as compared to the marketed formulation (81.4 ± 1.11 µg/cm2) after 8 hours indicating localized and sustained drug action that can be useful in treating acne vulgaris. The safety of optimized Adapalene gel determined by skin irritation studies performed on Sprague Dawley rats showed no irritation potential. Conclusion: Microparticles can provide promising carrier systems to deliver Adapalene, improving patient compliance due to enhanced skin deposition, localized and sustained action with reduced associated irritant effects.

Modulating the solubility of sulfacetamide by means of cocrystals

CrystEngComm ◽  
2014 ◽  
Vol 16 (26) ◽  
pp. 5859-5869 ◽  
Author(s):  
N. Rajesh Goud ◽  
Ronaq Ali Khan ◽  
Ashwini Nangia
Keyword(s):  
Residence Time ◽  
Therapeutic Efficacy ◽  
Parent Drug ◽  
Good Stability ◽  
Antibacterial Drug ◽  
Potential Candidate ◽  
Lower Solubility ◽  
Site Of Action ◽  
Low Solubility

The antibacterial drug sulfacetamide was screened with pharmaceutically acceptable coformers to discover solid forms with low solubility. Cocrystals with INIC and CAF exhibited 0.64 and 0.68 times the IDR of the parent drug. SACT–CAF cocrystal with lower solubility and good stability is a potential candidate to increase the drug residence time at the site of action for improved therapeutic efficacy.

scholarly journals CURCUMIN LOADED CHITOSAN NANOPARTICLES FOR TOPICAL DELIVERY: FORMULATION DESIGN, IN VITRO EVALUATION, KINETICS AND STABILITY STUDIES

2021 ◽  
Vol 10 (2) ◽  
pp. 48-52
Author(s):  
J Adlin Jino Nesalin ◽  
Preethi Raj M N
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Chitosan Nanoparticles ◽  
In Vitro Release ◽  
Topical Delivery ◽  
Particle Size Analysis ◽  
Size Analysis ◽  
In Vitro Drug Release ◽  
Topical Gel

The main objective of this research is to evaluate a new approach for the preparation of bio adhesive nanoparticles and to design an innovative topical delivery system for curcumin which is able to enhance the drug anticancer activity. Curcumin encapsulated nanoparticles were prepared by ionic gelation method. The nanoparticles were found to be discrete, spherical with free-flowing properties and evaluated for particle size analysis, shape (scanning electron microscopy), drug encapsulation efficiency, FTIR, DSC studies and in vitro release performance. The best selected nanoparticles formulation (FS5, containing drug: polymer ratio 1:5) was incorporated into gels with a bio adhesive polymer. The Nanoencapsulated topical gels were evaluated for pH, spreadability, extrudability, viscosity, in vitro drug release, drug release kinetics, bio adhesion test, accelerated stability of selected gel formulation. In vitro drug release rate for selected Nanoencapsulated bio adhesive topical gel (FS3 gel, containing 1 % w/w of drug loaded nanoparticles and 0.6 % w/w of Carbopol 934) was found to control curcumin release over 12h. The results were then compared statistically and obtained a satisfactory correlation. Thus, in conclusion preparation protocol of Nanoencapsulated topical gel study may be adopted for a successful delivery of Curcumin for topical use.

scholarly journals Evaluation of diclofenac niosomal gel formulated with Grewia gum for topical delivery

2020 ◽  
Vol 17 (1) ◽  
pp. 13-18
Author(s):  
Christian A. Alalor ◽  
Peter E. Jokor
Keyword(s):  
Thin Film ◽  
Topical Delivery ◽  
Synthetic Polymer ◽  
Gelling Agent ◽  
Natural Polymer ◽  
Gelling Agents ◽  
Grewia Gum ◽  
Niosomal Gel ◽  
Gastric Irritation

The purpose of this study was to formulate niosomal gel for topical delivery of diclofenac using Grewia gum as gelling agent. Niosomes containing 1g of diclofenac were formed using the thin film hydration (TFH) method. Niosomal gels were then formulated using a semi-synthetic polymer, hydroxypropylmethylcellulose (HPMC) and a natural polymer, Grewia gum as gelling agents. The formulated gels were evaluated for spreadability, viscosity, extrudability, homogeneity, clarity and pH. Results show that gels having pH and viscosity ranges of 6.8-7.3 and 265-490 Poise respectively were formed. The gels were homogenous, clear and showed good spreadability and extrudability except for batches F7 and F8. The gels formulated using the test gum, Grewia gum compared favourably with those of the standard polymer, HPMC as well as with the marketed gel. Formulation F5 containing 2% w/w Grewia gum, the optimized batch, showed viscosity of 265 poise, pH of 6.9, spreadability and extrudability values of 5.55 cm and 5.00 g/s respectively. In conclusion, Grewia gum at a concentration of 2% w/w could be used in the formulation niosomal gel for the delivery of diclofenac, which would help to circumvent the potential gastric irritation of diclofenac when used orally. Keywords: Niosomes; Grewia gum; Diclofenac; Lipid hydration; Topical delivery

A nanoporous photosensitizing hydrogel based on chitosan cross-linked by zinc phthalocyanine: an injectable and pH-stimuli responsive system for effective cancer therapy

RSC Advances ◽  
2016 ◽  
Vol 6 (94) ◽  
pp. 91445-91452 ◽  
Author(s):  
Ali Reza Karimi ◽  
Azam Khodadadi ◽  
Mahnaz Hadizadeh
Keyword(s):  
Photodynamic Therapy ◽  
Cancer Therapy ◽  
Therapeutic Efficacy ◽  
Zinc Phthalocyanine ◽  
Stimuli Responsive ◽  
Zinc Phthalocyanines ◽  
Tumor Selectivity ◽  
Biological Environment ◽  
Low Solubility ◽  
Effective Cancer Therapy

Although zinc phthalocyanines (ZnPcs) have promising applications in photodynamic therapy (PDT), their therapeutic efficacy suffer from their low solubility in the biological environment and their lack of tumor selectivity.

scholarly journals Nanostructured Non-Ionic Surfactant Carrier-Based Gel for Topical Delivery of Desoximetasone

2021 ◽  
Vol 22 (4) ◽  
pp. 1535
Author(s):  
Parinbhai Shah ◽  
Benjamin Goodyear ◽  
Nirali Dholaria ◽  
Vinam Puri ◽  
Bozena Michniak-Kohn
Keyword(s):  
Drug Delivery ◽  
Skin Diseases ◽  
Skin Permeation ◽  
Topical Delivery ◽  
Gelling Agent ◽  
Oral Drug ◽  
Ionic Surfactant ◽  
Content Uniformity ◽  
Drug Bioavailability ◽  
Drug Content

Psoriasis is a chronic autoimmune skin disease impacting the population globally. Pharmaceutical products developed to combat this condition commonly used in clinical settings are IV bolus or oral drug delivery routes. There are some major challenges for effectively developing new dosage forms for topical use: API physicochemical nature, the severity of the disease state, and low bioavailability present challenges for pharmaceutical product developers. For non-severe cases of psoriasis, topical drug delivery systems may be preferred or used in conjunction with oral or parenteral therapy to address local symptoms. Elastic vesicular systems, termed “niosomes”, are promising drug delivery vehicles developed to achieve improved drug delivery into biological membranes. This study aimed to effectively incorporate a corticosteroid into the niosomes for improving the drug bioavailability of desoximetasone, used to treat skin conditions via topical delivery. Niosomes characterization measurements were drug content, pH, spreadability, specific gravity, content uniformity, rheology, and physicochemical properties. Formulations used a topical gelling agent, Carbomer 980 to test for in vitro skin permeation testing (IVPT) and accelerated stability studies. The developed niosomal test gel provided approximately 93.03 ± 0.23% to 101.84 ± 0.11% drug content with yield stresses ranging from 16.12 to 225.54 Pa. The permeated amount of desoximetasone from the niosomal gel after 24 h was 9.75 ± 0.44 µg/cm2 compared to 24.22 ± 4.29 µg/cm2 released from the reference gel tested. Furthermore, a drug retention study compared the test gel to a reference gel, demonstrating that the skin retained 30.88 ng/mg of desoximetasone while the reference product retained 26.01 ng/mg. A controlled drug release profile was obtained with a niosomal formulation containing desoximetasone for use in a topical gel formulation showing promise for potential use to treat skin diseases like psoriasis.

scholarly journals Biodegradable and Biocompatible Subcutaneous Implants Consisted of Ph-Sensitive Mebendazole-Loaded/Folic Acid-Targeted Chitosan Nanoparticles for Murine Triple-Negative Breast Cancer Treatment

2021 ◽  
Author(s):  
Amirhosein Kefayat ◽  
Maryam Hosseini ◽  
Fatemeh Ghahremani ◽  
mohammad rafienia
Keyword(s):  
Folic Acid ◽  
Oral Administration ◽  
Survival Time ◽  
Therapeutic Efficacy ◽  
Triple Negative ◽  
Chitosan Nanoparticles ◽  
High Dose ◽  
Blood Biochemical ◽  
Anti Cancer ◽  
Low Solubility

Abstract Background: Mebendazole (MBZ) is a well-known anti-parasite drug with significant anti-cancer properties. However, MBZ exhibits low solubility, limited absorption efficacy, extensive first-pass effect, and low bioavailability. Therefore, multiple oral administration of high dose MBZ is required daily for achieving the therapeutic serum level which can cause severe side effects and patients’ non-compliance. Method: In the present study, MBZ-loaded/folic acid-targeted chitosan nanoparticles (CS-FA-MBZ) were synthesized, characterized, and used to form cylindrical subcutaneous implants for 4T1 triple-negative breast tumor (TNBC) treatment in BALB/c mice. The therapeutic efficacy of the CS-FA-MBZ implants was investigated after subcutaneous implantation in comparison with Control (no-treatment), MBZ (40 mg/kg, oral administration, twice a week for 2 weeks), and CS-FA implants, according to 4T1 tumors’ growth progression, metastasis, and tumor-bearing mice survival time. Also, their biocompatibility was evaluated by blood biochemical analyzes and histopathological investigation of vital organs. Results: The CS-FA-MBZ implants were completely degraded 15 days after implantation and caused about 73.3%, 46.5%, 37.3% decrease in the mean tumors’ volume in comparison with the Control (1050.5±120.7 mm3), MBZ (561.7±70.3 mm3), and CS-FA (658.3±88.1 mm3) groups, respectively. Average liver metastatic colonies’ number per microscope field at the CS-FA-MBZ (8.6±1.9) group was significantly (P<0.05) lower than the Control (24.5±4.1), MBZ (14.1±2.5), and CS-FA (15.7±3.1) groups. In addition, the CS-FA-MBZ treated mice exhibited about 51%, 24%, and 17% more survival time (days) after the cancer cells injection in comparison with the Control, MBZ, and CS-FA groups, respectively. Moreover, the CS-FA-MBZ implants were completely biocompatible based on histopathology and blood biochemical analyzes. Conclusion: Taking together, CS-FA-MBZ implants were completely biodegradable and biocompatible with high therapeutic efficacy in a murine TNBC model.

scholarly journals Development of Topical Niosomal Gel of Benzoyl Peroxide

2011 ◽  
Vol 2011 ◽  
pp. 1-6 ◽  
Author(s):  
Jigar Vyas ◽  
Puja Vyas ◽  
Dhaval Raval ◽  
Paresh Paghdar
Keyword(s):  
Benzoyl Peroxide ◽  
In Vitro Release ◽  
Skin Penetration ◽  
Topical Gel ◽  
Different Temperatures ◽  
Skin Redness ◽  
The Stability ◽  
Niosomal Gel ◽  
Vitro Release

Benzoyl peroxide is macrolide antibiotic used commonly for the treatment of acne either alone or in combination. But it suffers from side effects like skin redness, irritation, itching, and edema. Niosomes, a nonionic surfactant vesicular formulation, have been explored extensively for topical application to enhance skin penetration as well as to improve skin retention of drugs. In the present study, Benzoyl peroxide was entrapped into niosomes by thin film hydration technique, and various process parameters were optimized by partial factorial design. The optimized niosomal formulation was incorporated into HPMC K15 gel and extensively characterized for percentage drug entrapment (PDE) and in vitro release performance. The stability of above formulation was studied at different temperatures. The present study demonstrated prolongation of drug release, increased drug retention into skin, and improved permeation across the skin after encapsulation of benzoyl peroxide into niosomal topical gel.

scholarly journals Niosomal Gel of Lornoxicam for Topical Delivery: In vitro Assessment and Pharmacodynamic Activity

2013 ◽  
Vol 14 (3) ◽  
pp. 1072-1082 ◽  
Author(s):  
Deepak Kumbhar ◽  
Preeti Wavikar ◽  
Pradeep Vavia
Keyword(s):  
Topical Delivery ◽  
In Vitro Assessment ◽  
Niosomal Gel
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