Chronomodulated press-coated pulsatile therapeutic system for aceclofenac: optimization of factors influencing drug release and lag time

Patil, Sumit; Pund, Swati; Joshi, Amita; Shishoo, C. J.; Shahiwala, Aliasgar

doi:10.2147/cpt.s16504

Cited by 11 publications

(7 citation statements)

References 26 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The two dotted reference lines represent the experimental variance ( Figure 3 A,C,E,G). The probability of each active effect is represented graphically as box plots and coefficients of Bayesian analysis were also calculated ( Figure 3 B,D,F,H) [ 46 ].…”

Section: Resultsmentioning

confidence: 99%

Formulation-by-Design of Efinaconazole Spanlastic Nanovesicles for Transungual Delivery Using Statistical Risk Management and Multivariate Analytical Techniques

2022

View full text Add to dashboard Cite

As regulatory and technical landscapes for pharmaceutical formulation development are rapidly evolving, a risk-management approach using multivariate analysis is highly essential for designing a product with requisite critical quality attributes (CQA). Efinaconazole, a newly approved poorly water-soluble antifungal triazole drug has poor permeability. Spanlastics, new-generation surfactant nanovesicles, being fluidic, help improve the permeability of drugs. Therefore, we optimized efinaconazole spanlastics using the concepts of Formulation-by-Design (FbD) and explored the feasibility of transungual delivery for the management of onychomycosis. Using the Ishikawa fishbone diagram, the risk factors that may have an impact on the CQA of efinaconazole spanlastic vesicles were identified. Application of the Plackett–Burman experimental design facilitated the screening of eight different formulation and process parameters influencing particle size, transmittance, relative deformability, zeta potential, entrapment efficiency, and dissolution efficiency. With the help of Pareto charts, the three most significant factors were identified, viz., vesicle builder (Span), edge activator (Tween), and mixing time. The levels of these three critical variables were optimized by FbD to reduce the particle size and maximize the transparency, relative deformability, encapsulation efficiency, and dissolution efficiency of efinaconazole spanlastic nanovesicles. Bayesian and Lenth’s analysis and mathematical modeling of the experimental data helped to quantify the critical formulation attributes required for getting the formulation with optimum quality features. The optimized efinaconazole-loaded spanlastic vesicles had a particle size of 197 nm, transparency of 91%, relative deformability of 12.5 min, and dissolution efficiency of 81.23%. The spanlastic formulation was incorporated into a gel and explored ex vivo for transungual delivery. This explorative study provides an example of the application of principles of risk management, statistical multivariate analysis, and the FbD approach in developing efinaconazole spanlastic nanovesicles.

show abstract

Section: Resultsmentioning

confidence: 99%

Formulation-by-Design of Efinaconazole Spanlastic Nanovesicles for Transungual Delivery Using Statistical Risk Management and Multivariate Analytical Techniques

2022

View full text Add to dashboard Cite

show abstract

“…The low magnitudes of the bias values indicated a reasonable agreement between the predicted and the experimental values. It also indicated the robustness and high degree of predictive power of the generated quantitative mathematical models [21][22][23] . From the results obtained, it could be concluded that the generated Eqns.…”

Section: Table 5: All Responses Y1 To Y3 Along With Percent Error Formentioning

confidence: 88%

Formulation and Development of Gastroretentive Dipyridamole Microspheres: Proof of Concept by In vitro-In vivo Assessment

Vanshiv¹,

Joshi²,

Aware³

2018

pharmaceutical-sciences

View full text Add to dashboard Cite

Vanshiv, et al.: Gastroretentive Dipyridamole MicrospheresThe present research was aimed at development and optimization of dipyridamole gastroretentive microspheres. Gastro retention was achieved using swellable polymeric material such as hydroxypropyl methylcellulose K4M, ethyl cellulose as release retardant using solvent diffusion evaporation method. 3 2 factorial design was applied for the development of best optimized formulation. The design was developed by considering two independent variables, ethyl cellulose, and stirring speed. Their effect on drug release, entrapment efficiency, particle size was analysed using response surface methodology. Formulation B1 among all formulations tested was found to be the best as it demonstrated prolonged floating time, maximum entrapment efficiency and drug release in a controlled manner. Formulation B1 was characterized further for presence of residual solvent by gas chromatography/mass spectrometry and the result showed absence of residual solvent. Gastro retention was assessed using the in vivo gamma scintigraphy technique in albino rabbits and the results indicated prolonged gastric retention. Pharmacokinetic study comparing pure dipyridamole and dipyridamole microspheres was conducted and C max , T max and K el were estimated. In vitro-in vivo correlation was determined using Wagner-Nelson function. Pharmacokinetic study revealed improved bioavailability (30 %) as compared to pure dipyridamole. Good correlation was obtained with a regression coefficient of 0.9704. The in vivo gamma scintigraphy and pharmacokinetic studies confirmed gastric retention of the prepared dipyridamole floating microspheres. Accelerated stability studies indicated integrity of the developed formulations.

show abstract

“…Arthritis Pain in the morning and more pain in the night NSAIDS, glucocorticoids [59,60] Diabetes mellitus Increase in blood sugar level after meal Sulfonyl urea, insulin, bioguanide [61].…”

Section: Transdermal Devicementioning

confidence: 99%

Chronotherapeutic Drug Delivery Systems

Shanmugan¹,

Ramu²,

ameedi³

2015

J Drug Metab Toxicol

View full text Add to dashboard Cite

Recent advances in chronotherapeutics led to the development of pulsatile drug delivery systems which effectively delivered the drug at specified time. Diseases like asthma, arthritis, cancer, diabetes, hypertension, ulcer, hypercholesterolemia, congestive heart failure, stroke etc. show different day night pattern in onset and symptoms exacerbation. Pulsatile drug delivery systems deliver the drug at right time in desired levels providing the multiple benefits over the conventional dosage forms. According to the circadian rhythms of the body drug is facilitated to completely release after a lag time especially for drugs eliciting higher first pass effect and where nocturnal dosing is required these systems are highly beneficial. This review epitomizes the special focus on chronotherapeutics, various approaches in chronotherapeutic drug delivery and applications.

show abstract

Chronomodulated press-coated pulsatile therapeutic system for aceclofenac: optimization of factors influencing drug release and lag time

Cited by 11 publications

References 26 publications

Formulation-by-Design of Efinaconazole Spanlastic Nanovesicles for Transungual Delivery Using Statistical Risk Management and Multivariate Analytical Techniques

Formulation-by-Design of Efinaconazole Spanlastic Nanovesicles for Transungual Delivery Using Statistical Risk Management and Multivariate Analytical Techniques

Formulation and Development of Gastroretentive Dipyridamole Microspheres: Proof of Concept by In vitro-In vivo Assessment

Chronotherapeutic Drug Delivery Systems

Contact Info

Product

Resources

About