Development and Evaluation of Ketoconazole Loaded Nano-sponges for Topical Drug Delivery

2018 ◽  
Vol 11 (4) ◽  
pp. 4154-4162
Author(s):  
Harshal A. Pardeshi ◽  
Makarand S Gambhire ◽  
Kishore N. Gujar ◽  
Aniket A Vaidhya
Keyword(s):  
Drug Delivery ◽  
Antifungal Activity ◽  
Drug Release ◽  
Ex Vivo ◽  
Skin Permeation ◽  
Controlled Drug Release ◽  
Topical Drug Delivery ◽  
Molar Ratios ◽  
Skin Targeting ◽  
Skin Retention

Beta-cyclodextrin nanosponges (NS) based hydrogel had been studied as a topical delivery of ketoconazole (KTZ) for effective eradication of cutaneous fungal infection. The purpose of the present study was to develop KTZ loaded NS for topical drug delivery with skin targeting to minimizing the adverse side effects and providing a controlled release. The four types of NS were synthesized by varying the molar ratios of β-cyclodextrin (β-CD) to diphenylcarbonate (DPC) as a cross linker viz. 1:2, 1:4, 1:6, and 1:8. The KTZ loaded NS shows particle size 274.6-367 nm and high loading efficacy was obtained, FTIR, DSC, XRD studies confirmed the complexation of KTZ with NS. Hydrogel were evaluated comparatively with commercial product with respect to physicochemical properties, ex-vivo skin permeation and skin retention on human cadaver skin and antifungal activity. Ex-vivo study of KTZ-NS hydrogel exhibited controlled drug release up to 8 hrs whereas skin retention studies show avoidance of the systemic uptake and better accumulative uptake of the drug compared to marketed formulation. The zone of inhibition of KTZ-NS hydrogel was higher in comparison with commercial formulation against Candida albicans. These results indicate that the KTZ-NS is having controlled drug release, potential of skin targeting with enhanced antifungal activity.

scholarly journals FORMULATION AND IN VITRO CHARACTERISATION OF SOYBEAN OIL-HPMCK4M BASED BIGEL MATRIX FOR TOPICAL DRUG DELIVERY

2019 ◽  
pp. 33-38
Author(s):  
SHUBHAM MUKHERJEE ◽  
SUTAPA BISWAS MAJEE ◽  
GOPA ROY BISWAS
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Soybean Oil ◽  
Skin Permeation ◽  
Topical Drug Delivery ◽  
Zero Order Kinetics ◽  
Wide Range ◽  
Span 60 ◽  
Hydrophilic Gel

Objective: Hydrogels with scope for utilization in numerous fields possess limited applications due to problems in incorporating wide range of drugs and crossing the lipophilic barrier of the skin. Attempts to overcome these problems by developing organogel hold drawbacks. Challenges posed by drug lipophilicity or skin permeation can be solved by developing bigel formed via combination of lipophilic and hydrophilic gel phases in a definite proportion. The objective of the present study is to formulate and characterize matrix type bigel of soybean oil and HPMCK4M for topical drug delivery. Methods: Four batches of bigels were developed with two organogel formulations of soybean oil containing 20 and 22% w/v Span 60. Both organogels and bigels were examined for compatibility by FTIR spectroscopy, hemocompatibility and characterized for physical appearance, pH, rheological behavior and in vitro drug release pattern. Results: FTIR study confirmed compatibility between paracetamol and components of organogel or bigel. The oily feel of organogels disappeared with bigels which possessed a creamy and smooth texture. Pseudoplastic behaviour was confirmed by Ostwald-de wale power-law model in both organogels and bigels. Improved drug release was observed in bigel (BG1) formulation containing 3%w/v HPMCK4M and soybean oil based organogel with 20% w/v Span 60 as compared to the corresponding organogel (OG1). Organogels were foundto follow either zero-order kinetics (OG1) or Korsmeyer-Peppasmodel (OG2) while the formation of matrix was exhibited in bigels with drug diffusion predominantly of non-Fickian type. Conclusion: Therefore, bigels of soybean oil based organogel with HPMCK4M hydrogel formed gel matrix demonstrating improved drug release for topical application compared to organogel.

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.

Formulation, Optimization, and Evaluation of Ketoconazole Loaded Nanostructured Lipid Carrier Gel for Topical Delivery

2020 ◽  
Vol 10 (1) ◽  
pp. 61-71 ◽  
Author(s):  
Hemant A. Ranpise ◽  
Kishore N. Gujar ◽  
Sachin C. Pawar ◽  
Rajendra Awasthi ◽  
Kamal Dua ◽  
...  
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Skin Permeation ◽  
Thermal Studies ◽  
Average Particle Size ◽  
Topical Delivery ◽  
Nanostructured Lipid Carriers ◽  
Average Particle ◽  
Nanostructured Lipid Carrier ◽  
Skin Targeting

Objective: Ketoconazole is used in the treatment of superficial and systemic fungal infections. It acts by blocking the synthesis of ergosterol, an essential component of the fungal cell membrane. The purpose of this work was to formulate ketoconazole loaded nanostructured lipid carriers formulation for skin targeting to minimize the adverse side effects and to prolong release. Methods: The ketoconazole loaded nanostructured lipid carriers were optimized using 32 factorial design to evaluate the effects of process and formulation variables. The nanostructured lipid carriers were prepared by melt-dispersion ultra-sonication method. The formulations were finally incorporated into polymeric gels of Carbopol 940 for convenient application. The gels were evaluated comparatively with commercially available formulations of ketoconazole with respect to ex vivo skin permeation and deposition study on human cadaver skin. Results: Nanostructured lipid carriers showed average particle size, zeta potential, and percentage entrapment in the range of 125.8 ± 1.8 to 295.0 ± 3.8 nm, -13.2 ± 1.1 to -30.9 ± 2.2 mV, and 69.47 ± 2.8 to 95.49 ± 4.5, respectively. Thermal studies revealed no drug-excipient incompatibility and amorphization of ketoconazole. Ex vivo study of the gel exhibited prolonged drug release up to 12 h. In vitro drug deposition study showed that the gel formulation can avoid the systemic uptake, better accumulative uptake of the drug, and nonirritant to the skin compared to marketed formulation. Optimized formulation exhibited better antifungal activity when compared to ketoconazole loaded gel and marketed cream (Keto ® cream). Histolopathology results indicated no toxic effect on the skin. Conclusion: These results indicate that developed nanostructured lipid-carriers gel formulation represents a promising carrier for topical delivery of ketoconazole, having controlled drug release, and potential of skin targeting.

Nanostructured lipid carrier-incorporated gel for efficient topical delivery of fluconazole

2021 ◽  
Author(s):  
Archana Patil ◽  
Vedangi Tuencar ◽  
Anand Gadad ◽  
Panchaxari Dandagi ◽  
Rajashree Masareddy
Keyword(s):  
Drug Delivery ◽  
Ex Vivo ◽  
Skin Permeation ◽  
Entrapment Efficiency ◽  
Nanostructured Lipid Carrier ◽  
Topical Drug Delivery ◽  
In Vitro Drug Release ◽  
Drug Permeability ◽  
Permeation Studies

Background: Nanostructured lipid carriers (NLCs) of fluconazole were prepared to improve permeability and thereby effective topical drug delivery. Materials and method: NLCs were prepared and evaluated, and then the optimized NLC suspension was incorporated into a gel that was further evaluated for topical drug delivery. Results and discussion: F-2 NLC formulation was optimized based on results of particle size (161.3 ± 1.385 nm), polydispersity index (0.401), zeta potential (-33 ± 0.46), entrapment efficiency (82.26 ± 0.91%) and in vitro drug release (76.40 ± 0.21%). Ex vivo skin permeation studies showed flux of F-2 gel and the comparison marketed gel as 0.21 and 0.18 mg/cm2/h, respectively. The in vitro antifungal study revealed significantly better activity compared with the marketed gel. Conclusion: Fluconazole NLCs increase drug permeability and proved to be effective in topical drug delivery.

Nanostructured Ketorolac-Tromethamine/MCF: Synthesis, Characterization and Application in Drug Release System

2018 ◽  
Vol 14 (5) ◽  
pp. 432-439 ◽  
Author(s):  
Juliana M. Juarez ◽  
Jorgelina Cussa ◽  
Marcos B. Gomez Costa ◽  
Oscar A. Anunziata
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Therapeutic Efficacy ◽  
Drug Delivery Systems ◽  
Controlled Drug Release ◽  
Delivery Systems ◽  
The Body ◽  
Fickian Diffusion ◽  
Ketorolac Tromethamine

Background: Controlled drug delivery systems can maintain the concentration of drugs in the exact sites of the body within the optimum range and below the toxicity threshold, improving therapeutic efficacy and reducing toxicity. Mesostructured Cellular Foam (MCF) material is a new promising host for drug delivery systems due to high biocompatibility, in vivo biodegradability and low toxicity. Methods: Ketorolac-Tromethamine/MCF composite was synthesized. The material synthesis and loading of ketorolac-tromethamine into MCF pores were successful as shown by XRD, FTIR, TGA, TEM and textural analyses. Results: We obtained promising results for controlled drug release using the novel MCF material. The application of these materials in KETO release is innovative, achieving an initial high release rate and then maintaining a constant rate at high times. This allows keeping drug concentration within the range of therapeutic efficacy, being highly applicable for the treatment of diseases that need a rapid response. The release of KETO/MCF was compared with other containers of KETO (KETO/SBA-15) and commercial tablets. Conclusion: The best model to fit experimental data was Ritger-Peppas equation. Other models used in this work could not properly explain the controlled drug release of this material. The predominant release of KETO from MCF was non-Fickian diffusion.

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.

Functionally Tailored Electro-Sensitive Poly(Acrylamide)-g-Pectin Copolymer Hydrogel for Transdermal Drug Delivery Application: Synthesis, Characterization, In-vitro and Ex-vivo Evaluation

2020 ◽  
Vol 10 (3) ◽  
pp. 185-196
Author(s):  
Sudha B. Patil ◽  
Syed Z. Inamdar ◽  
Kakarla R. Reddy ◽  
Anjanapura V. Raghu ◽  
Krishnamachari G. Akamanchi ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Transdermal Drug Delivery ◽  
Ex Vivo ◽  
Transmission Rate ◽  
Electric Signal ◽  
Poly Vinyl Alcohol ◽  
Electric Stimulus ◽  
Copolymer Hydrogel ◽  
Transdermal Drug Delivery Systems

Background and Objectives: To develop electro-sensitive transdermal drug delivery systems (ETDDS) using polyacrylamide-grafted-pectin (PAAm-g-PCT) copolymer hydrogel for rivastigmine delivery. Methods: Free radical polymerization and alkaline hydrolysis technique was employed to synthesize PAAm-g-PCT copolymer hydrogel. The PAAm-g-PCT copolymeric hydrogel was used as a reservoir and cross-linked blend films of PCT and poly(vinyl alcohol) as rate-controlling membranes (RCMs) to prepare ETDDS. Results: The pH of the hydrogel reservoir was found to be in the range of 6.81 to 6.93 and drug content was 89.05 to 96.29%. The thickness of RCMs was in the range of 51 to 99 μ and RCMs showed permeability behavior against water vapors. There was a reduction in the water vapor transmission rate as the glutaraldehyde (GA) concentration was increased. The drug permeation rate from the ETDDS was enhanced under the influence of electric stimulus against the absence of an electric stimulus. The increase in flux by 1.5 fold was recorded with applied electric stimulus. The reduction in drug permeability observed when the concentration of GA was increased. Whereas, the permeability of the drug was augmented as an electric current was changed from 2 to 8 mA. The pulsatile drug release under “on– off” cycle of electric stimulus witnessed a faster drug release under ‘on’ condition and it was slow under ‘off’ condition. The alteration in skin composition after electrical stimulation was confirmed through histopathology studies. Conclusion: The PAAm-g-PCT copolymer hydrogel is a useful carrier for transdermal drug delivery activated by an electric signal to provide on-demand release of rivastigmine.

NIR responsive AuNRs/pNIPAM/PEGDA inverse opal hydrogel microcarriers for controllable drug delivery

2021 ◽  
Author(s):  
Lingzi Liu ◽  
Xiaoyan Sun ◽  
Baofen Ye ◽  
Zhengyu Yan
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Delivery System ◽  
Gold Nanorods ◽  
Controlled Drug Release ◽  
Inverse Opal

Particle-based delivery system has merged as a powerful platform in controlled drug release. The present study developed a new inverse opal hydrogel microcarriers system composed of gold nanorods (AuNRs) for...

A general method to greatly enhance ultrasound-responsiveness for common polymeric assemblies

2020 ◽  
Vol 11 (19) ◽  
pp. 3296-3304
Author(s):  
Jinkang Dou ◽  
Ruiqi Yang ◽  
Kun Du ◽  
Li Jiang ◽  
Xiayun Huang ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Controlled Drug Delivery ◽  
Controlled Drug Release ◽  
Promising Technique ◽  
Polymeric Assemblies ◽  
General Method

Ultrasound-controlled drug release is a very promising technique for controlled drug delivery due to the unique advantages of ultrasound as the stimulus.

scholarly journals CHEMICAL MODIFICATION, CHARACTERIZATION AND EVALUATION OF MUCOADHESIVE POTENTIALITY OF ASSAM BORA RICE STARCH

2017 ◽  
Vol 9 (9) ◽  
pp. 132 ◽  
Author(s):  
Abdul Baquee Ahmed ◽  
Iman Bhaduri
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Sustained Release ◽  
Chemical Modification ◽  
Ex Vivo ◽  
Rice Starch ◽  
Modified Starch ◽  
Native Starch ◽  
Ft Ir

Objective: The objective of the present study was to chemical modification, characterization and evaluation of mucoadhesive potentiality of Assam bora rice starch as potential excipients in the sustained release drug delivery system. Methods: The starch was isolated from Assam bora rice and esterified using thioglycolic acid and characterized by Fourier transform infrared spectroscopy (FT-IR), Differential scanning calorimetry (DSC) and Nuclear magnetic resonance (NMR). The 10% w/v gel formulation based on modified bora rice starch loaded with irinotecan (0.6%) was prepared and evaluated for various rheological properties, ex-vivo mucoadhesion using goat intestine and in vitro drug release study in phosphate buffer pH 6.8.Results: The chemical modification was confirmed by FT-IR and NMR studies with the presence of the peak at 2626.74 cm-1 and a singlet at 2.51 respectively due to–SH group. Ex-vivo mucoadhesion studies showed 6.6 fold increases in mucoadhesion of the modified starch with compared to native starch (46.3±6.79g for native starch; 308.7±95.31g for modified starch). In vitro study showed 89.12±0.84 % of drug release after 6 h in phosphate buffer pH 6.8 and the release kinetics followed Non-Fickian diffusion.Conclusion: The modified Assam bora rice starch enhanced a mucoadhesive property of the native starch and thus, can be explored in future as a potential excipient for the sustained release mucoadhesive drug delivery system.

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