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 FORMULATION AND EVALUATION OF GASTRORETENTIVE DRUG DELIVERY SYSTEM CONTAINING COMBINATION OF GLIPIZIDE AND METFORMIN HYDROCHLORIDE

2016 ◽  
Vol 9 (6) ◽  
pp. 235
Author(s):  
Vidya Peter
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
In Vitro Dissolution ◽  
Oral Drug ◽  
Metformin Hydrochloride ◽  
Special Focus ◽  
Content Uniformity ◽  
Drug Bioavailability ◽  
Gastro Retentive

The purpose of gastro-retentive drug delivery systems was special focus on the principle mechanism of floatation to achieve gastric retention. The objective is to develop a gastro-retentive drug delivery system of Glipizide and Metformine hydrochloride is to overcome the biggest problem in oral drug delivery is low and erratic drug bioavailability. Glipizide and Metformine hydrochloride are used for the treatment of diabetes mellitus. Seven formulations containing retardant material and alkalizing agent were prepared with solubilizing agent in different ratio. The ability of various polymers to retain the drug when used in different concentrations was investigated. It was found that sodium bicarbonate reacts with HCl and produce CO2 which creates pores in tablet and elevates swelling by wetting polymer. So it helps in maintaining the buoyancy. The release rate could be modified by varying the polymer ratio, concentration of alkalizing and solubilizing agent. The prepared tablets were evaluated for general appearance, content uniformity, hardness, friability, buoyancy and in vitro dissolution studies.

Formulation, Optimization,and Ex-Vivo Evaluation of Novel Lipid Carriers for Enhanced Transdermal Delivery of Hydroquinone

2020 ◽  
Vol 12 ◽  
Author(s):  
Shivani Verma ◽  
Sukhjinder Kaur ◽  
Lalit Kumar
Keyword(s):  
Ex Vivo ◽  
Skin Permeation ◽  
Topical Delivery ◽  
Gelling Agent ◽  
Minimum Size ◽  
Prolonged Release ◽  
Freeze Dried ◽  
Ft Ir ◽  
Ir Analysis ◽  
Skin Retention

Background: HQ is used for hyper-pigmentation treatment using conventional creams and gels. These formulations show various disadvantages like poor skin permeation, allergic reactions, and repeated use decreasing patient compliance. Objectives: The present work involved formulation, statistical optimization, and characterization of nanostructured lipid carriers (NLCs) for efficient topical delivery of hydroquinone (HQ) for hyperpigmentation treatment. Methods: The NLCs were optimized exploring Box–Behnken design (BBD) using three independent variables and two dependent variables. Formulation having the minimum size and maximum drug entrapment was considered as optimized formulation. Optimized formulation was evaluated for drug release followed by its freeze-drying. The freeze-dried formulation was subjected to differential scanning calorimetry (DSC) analysis, X-raydiffraction (XRD) analysis, and Fourier transform-infrared spectroscopy (FT-IR) analysis. Furthermore, NLCs based gel was prepared by using Carbopol 934 as a gelling agent. NLCs based gel was evaluated for skin permeation, skin retention, and skin distribution (through confocal microscopic analysis) using pig ear skin. Results: Optimized NLCs showed smaller particle size [(271.9 ± 9) nm], high drug entrapment [(66.4 ± 1.2) %], tolerable polydispersity index (PDI) (0.221 ± 0.012), and zeta potential [(-25.9± 1.2) mV]. The FT-IR analysis revealed excellent compatibility between HQ and other excipients. The Carbopol 934 gel containing NLCs showed high transdermal flux [(163 ± 16.2) μg/cm2/h], permeability coefficient (0.0326 ± 0.0016), and skin permeation enhancement ratio (3.7 ± 0.4) compared to marketed cream of HQ. The results of confocal microscopic (CLSM) analysis revealed the accumulation of optimized NLCs in the lower epidermal layers of skin. Conclusion: NLCs based gel was considered effective in the topical delivery of HQ to treat hyper-pigmentation due high skin permeation, skin retention, and prolonged release of HQ.

scholarly journals Niosomes: Potential Nanocarriers for Drug Delivery

2020 ◽  
Vol 11 (03) ◽  
pp. 389-394
Author(s):  
Ashish Suttee ◽  
Vijay Mishra ◽  
Pallavi Nayak ◽  
Manvendra Singh ◽  
Pavani Sriram
Keyword(s):  
Drug Delivery ◽  
Delivery System ◽  
Scale Up ◽  
Production Costs ◽  
Ionic Surfactant ◽  
Drug Bioavailability ◽  
Pharmacological Agents ◽  
Drug Degradation ◽  
Advantages And Disadvantages ◽  
Traditional Drug

Niosomes are novel vesicular drug delivery systems, where the solution is surrounded by non-ionic surfactant vesicles. The niosomes offer different benefits over the traditional drug delivery system. Niosomes are structurally similar to liposomes, as they also consist of a bilayer. In the case of niosomes, the bilayer consists of non-ionic surface-active agents instead of phospholipids, as seen in liposomes. Niosomes are much more stable during the process of formulation and storage, as compared to liposomes. Niosomes may resolve the issues of insolubility, volatility, poor bioavailability, and rapid drug degradation. It has been discovered in recent years that, these vesicles can enhance drug bioavailability and can act as a new strategy to deliver many conventional therapeutic agents, such as, protein drugs, and gene materials. It is also easy to prepare and scale up this novel delivery system with low production costs. The delivery of drugs via niosomal formulations may be relevant to several pharmacological agents for their activity against different diseases. The present review provides an overview about the advantages and disadvantages, fabrication techniques, types, characterization technique, and different applications of niosomes.

scholarly journals Formulation and Characterization of Cefixime Phytosomes for Oral Drug Delivery

1970 ◽  
Vol 7 (5) ◽  
pp. 65-73
Author(s):  
Saloni Jain ◽  
Rahul Ancheriya ◽  
S Srivastva ◽  
Shankar Lal Soni ◽  
Mukesh Sharma
Keyword(s):  
Drug Delivery ◽  
Oral Drug Delivery ◽  
Biological Activities ◽  
Herbal Medicines ◽  
Memory Loss ◽  
Oral Drug ◽  
Target Tissue ◽  
Drug Bioavailability ◽  
Age Related ◽  
Health Promoting

Novel drug delivery systems (NDDS) are one of the most strategies which enable to overcome the problems related to drug bioavailability. It is the rate and extent to which a drug becomes available to the target tissue after its administration. Over the last century, phyto-chemical science and phyto-pharmacological science established numerous plant compounds with various biological activities and health promoting benefits such as anti-mutagenicity, anti-carcinogenicity and anti-oxidative activity, for age-related diseases namely memory loss, osteoporosis, diabetic wounds, immune and liver disorders, etc. Herbal medicines have been known since eons for their safety, efficacy, folk acceptability and fewer side effects.  

scholarly journals Development and Evaluations of Transdermally Delivered Luteolin Loaded Cationic Nanoemulsion: In Vitro and Ex Vivo Evaluations

Pharmaceutics ◽  
2021 ◽  
Vol 13 (8) ◽  
pp. 1218
Author(s):  
Mohammad A. Altamimi ◽  
Afzal Hussain ◽  
Sultan Alshehri ◽  
Syed Sarim Imam ◽  
Usamah Abdulrahman Alnemer
Keyword(s):  
Drug Release ◽  
Zeta Potential ◽  
Transdermal Delivery ◽  
Ex Vivo ◽  
Skin Permeation ◽  
Oral Drug ◽  
In Vitro Drug Release ◽  
Drug Deposition ◽  
Drug Content

Introduction: Luteolin (LUT) is natural flavonoid with multiple therapeutic potentials and is explored for transdermal delivery using a nanocarrier system. LUT loaded cationic nanoemulsions (CNE1–CNE9) using bergamot oil (BO) were developed, optimized, and characterized in terms of in vitro and ex vivo parameters for improved permeation. Materials and methods: The solubility study of LUT was carried out in selected excipients, namely BO, cremophor EL (CEL as surfactant), labrasol (LAB), and oleylamine (OA as cationic charge inducer). Formulations were characterized with globular size, polydispersity index (PDI), zeta potential, pH, and thermodynamic stability studies. The optimized formulation (CNE4) was selected for comparative investigations (% transmittance as %T, morphology, chemical compatibility, drug content, in vitro % drug release, ex vivo skin permeation, and drug deposition, DD) against ANE4 (anionic nanoemulsion for comparison) and drug suspension (DS). Results: Formulations such as CNE1–CNE9 and ANE4 (except CNE6 and CNE8) were found to be stable. The optimized CNE4 based on the lowest value of globular size (112 nm), minimum PDI (0.15), and optimum zeta potential (+26 mV) was selected for comparative assessment against ANE4 and DS. The %T values of CNE1–CNE9 were found to be ˃95% and CEL content slightly improved the %T value. The spherical CNE4 was compatible with excipients and showed % total drug content in the range of 97.9–99.7%. In vitro drug release values from CNE4 and ANE4 were significantly higher than DS. Moreover, permeation flux (138.82 ± 8.4 µg/cm2·h), enhancement ratio (8.23), and DD (10.98%) were remarkably higher than DS. Thus, ex vivo parameters were relatively high as compared to DS which may be attributed to nanonization, surfactant-mediated reversible changes in skin lipid matrix, and electrostatic interaction of nanoglobules with the cellular surface. Conclusion: Transdermal delivery of LUT can be a suitable alternative to oral drug delivery for augmented skin permeation and drug deposition.

Unmet Quality Needs in Oral Drug Delivery: Contrasts of Drug Content and Uniformity on Distinct Approaches for Achieving Individual Dosing

2019 ◽  
Vol 20 (8) ◽  
Author(s):  
Jaqueline Kalleian Eserian ◽  
Márcia Lombardo ◽  
Jair Ribeiro Chagas ◽  
José Carlos Fernandes Galduróz
Keyword(s):  
Drug Delivery ◽  
Oral Drug Delivery ◽  
Oral Drug ◽  
Drug Content

Topical Drug Delivery of Anti-infectives Employing Lipid-Based Nanocarriers: Dermatokinetics as an Important Tool

2019 ◽  
Vol 24 (43) ◽  
pp. 5108-5128 ◽  
Author(s):  
Kanika Thakur ◽  
Gajanand Sharma ◽  
Bhupindar Singh ◽  
Om Prakash Katare
Keyword(s):  
Drug Delivery ◽  
Infectious Diseases ◽  
Patient Compliance ◽  
Skin Permeation ◽  
Skin Penetration ◽  
Topical Delivery ◽  
Controlled Drug Release ◽  
Topical Drug Delivery ◽  
Promising Strategy ◽  
Drug Resistant Strains

Background:The therapeutic approaches for the management of topical infections have always been a difficult approach due to lack of efficacy of conventional topical formulations, high frequency of topical applications and non-patient compliance. The major challenge in the management of topical infections lies in antibiotic resistance which leads to severe complications and hospitalizations resulting in economic burden and high mortality rates.Methods:Topical delivery employing lipid-based carriers has been a promising strategy to overcome the challenges of poor skin permeation and retention along with large doses which need to be administered systemically. The use of lipid-based delivery systems is a promising strategy for the effective topical delivery of antibiotics and overcoming drug-resistant strains in the skin. The major systems include transfersomes, niosomes, ethosomes, solid lipid nanoparticles, nanostructured lipid carriers, microemulsion and nanoemulsion as the most promising drug delivery approaches to treat infectious disorders. The main advantages of these systems include lipid bilayer structure which mimics the cell membrane and can fuse with infectious microbes. The numerous advantages associated with nanocarriers like enhanced efficacy, improvement in bioavailability, controlled drug release and ability to target the desired infectious pathogen have made these carriers successful.Conclusion:Despite the number of strides taken in the field of topical drug delivery in infectious diseases, it still requires extensive research efforts to have a better perspective of the factors that influence drug permeation along with the mechanism of action with regard to skin penetration and deposition. The final objective of the therapy is to provide a safe and effective therapeutic approach for the management of infectious diseases affecting topical sites leading to enhanced therapeutic efficacy and patient-compliance.

Self-emulsifying Drug Delivery System Improve Oral Bioavailability: Role of Excipients and Physico-chemical Characterization

2020 ◽  
Vol 8 (4) ◽  
pp. 290-301
Author(s):  
Yujin Zhu ◽  
Jing Ye ◽  
Quan Zhang
Keyword(s):  
Drug Delivery ◽  
Physicochemical Property ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Bioavailability ◽  
Water Soluble ◽  
Oral Drug ◽  
Scale Production ◽  
Drug Bioavailability

: Self-emulsifying drug delivery system (SEDDS) is a kind of solid or liquid formulation composed of drugs, oil, surfactant and cosurfactant. It could form a fine emulsion (micro/nano) in the gastrointestinal tract after oral administration. Later on, the formed emulsion is absorbed through the lymphatic pathway. The oral bioavailability of drugs in SEDDS would be improved for bypassing the first-pass effect of the liver. Therefore, SEDDS has become a vital strategy to increase the oral bioavailability of poor watersoluble drugs. In addition, there is no aqueous phase in SEDDS, thus SEDDS is a homogeneous system, consequently being suitable for large-scale production and more stable than conventional emulsion. However, the role of formulation aspects in the biological property of SEDDS is not fully clear. In order to prepare the satisfying SEDDS to improve oral drug bioavailability, we need to fully understand the various factors that affect the in vivo behavior of SEDDS. In this review, we would explore the role of ingredient (drugs, oils, surfactant and cosurfactant) of SEDDS in increasing oral drug bioavailability. We would also discuss the effect of physicochemical property (particle size and zeta potential) of SEDDS on the oral drug bioavailability enhancement. This review would provide an approach to develop a rational SEDDS to improving oral drug bioavailability. Lay Summary: Self-emulsifying drug-delivery system (SEDDS) has been proven to be promising in ameliorating the oral bioavailability of poor water-soluble drugs. This review highlighted the influence of excipients and physicochemical property of SEDDS on the formation of emulsion and the oral absorption of drugs in the body.

scholarly journals Advances in Oral Drug Delivery

2021 ◽  
Vol 12 ◽  
Author(s):  
Mohammed S. Alqahtani ◽  
Mohsin Kazi ◽  
Mohammad A. Alsenaidy ◽  
Muhammad Z. Ahmad
Keyword(s):  
Drug Delivery ◽  
Drug Administration ◽  
Drug Absorption ◽  
Oral Drug Delivery ◽  
Oral Route ◽  
Oral Drug ◽  
Drug Bioavailability ◽  
Oral Drug Absorption ◽  
Mucosal Permeability ◽  
Novel Drug

The oral route is the most common route for drug administration. It is the most preferred route, due to its advantages, such as non-invasiveness, patient compliance and convenience of drug administration. Various factors govern oral drug absorption including drug solubility, mucosal permeability, and stability in the gastrointestinal tract environment. Attempts to overcome these factors have focused on understanding the physicochemical, biochemical, metabolic and biological barriers which limit the overall drug bioavailability. Different pharmaceutical technologies and drug delivery systems including nanocarriers, micelles, cyclodextrins and lipid-based carriers have been explored to enhance oral drug absorption. To this end, this review will discuss the physiological, and pharmaceutical barriers influencing drug bioavailability for the oral route of administration, as well as the conventional and novel drug delivery strategies. The challenges and development aspects of pediatric formulations will also be addressed.

scholarly journals Preparation and assessment of ocular inserts containing sulbactum for controlled drug delivery

2020 ◽  
Vol 10 (1-s) ◽  
pp. 66-71
Author(s):  
Monika Dhaka ◽  
Rupa Mazumdar ◽  
Md Rafiul Haque
Keyword(s):  
Drug Delivery ◽  
Antibacterial Agent ◽  
Content Uniformity ◽  
Surface Ph ◽  
Drug Content ◽  
Controlled Drugs ◽  
Accelerated Stability ◽  
Folding Endurance ◽  
Alcohol Ethyl

Ocuserts or Ophthalmic inserts are sterile preparations containing drug as dispersion or as solution in the polymeric support. The sulbactum is highly used as antibacterial agent in combination with other antibacterial agent. This study aims to formulate novel sulbactum ocuserts to enhance patient compliance through providing controlled drugs release from polymeric matrix. Ocuserts were prepared by solvent-casting method using different polymers HPMC, K4M, Polyvinyl alcohol,ethyl cellulose as polymer gelatine and propylene glycol and dibutyl phthalate as plasticizer in different ratios. The prepared ocusters were physic-chemichally evaluated for their weight, thickness, drug content uniformity, surface pH, swelling index (SI) and folding endurance. The viscosity of the polymeric solution used for the formulations was determined using Brookfield viscometer. In-Vitro Drug Release study and Accelerated stability studies were also performed. The prepared ocuserts show uniform weight, thickness and drug content. Their surface pH was in the physiological range and showed acceptable folding endurance. HPMC formulas had higher SI values. Results of in-vitro testing for one of the prepared ocuserts shows slow release of drugs up to 24 hours. One of the prepared ocuserts is promising for once-daily effective and safe drug delivery system of sulbactum for glaucoma treatment. Keyword: Ocuserts, sulbactum, viscosity, Ophthalmic

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