Formulation and optimization of microsponge-loaded emulgel to improve the transdermal application of acyclovir—a DOE based approach

Gusai, Tejal; Dhavalkumar, Mori; Soniwala, Moinuddin; Dudhat, Kiran; Vasoya, Jaydip M.; Chavda, Jayant

doi:10.1007/s13346-020-00862-w

Cited by 29 publications

(9 citation statements)

References 33 publications

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“…Besides topical drug delivery, a microsponge delivery system was investigated for colon targeted drug delivery systems earlier, dispensing in capsule [1] and tablet [2]. In previous years, researchers prepared and characterised microsponges entrapping various types of drugs, such as 5 -FU [3,4]; antifungal drugs-ketoconazole, miconazole, fluconazole, terbinafin HCl [5][6][7], antihypertensive drugs-nebivolol, valsartan [8,9], an anti-inflammatory drugketoprofen [10], timolol, used for glaucoma [11], antiviral drugs-valcyclovir, acyclovir [12,13], anthelmintic drug-albendazole [14]. Commercially microsponge delivery system is gaining importance as dermal and cosmetic products.…”

Section: Introductionmentioning

confidence: 99%

“…Optimisation by QBD for preparing microparticulate systems is nowadays practised by formulation scientists, and optimised operating variables aid in scale-up design. To enhance reliability and reproducibility of the method, several investigators started attempting simple factorial design [29], Central Composite Design -RSM method by design expert software [1,11,13,16,[28][29][30][31]. They presented linear as well as quadratic models.…”

Section: Introductionmentioning

confidence: 99%

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WITHDRAWN: Optimization and Scale-up Methodology in Preparing Microsponge Loaded with 5-Fluorouracil (5-FU).

Halder

Poddar²,

Khanam

2021

Preprint

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The present investigation aims at developing models by response surface methodology (FCCCD) followed by the scale-up method in preparing control release microsponge particles loaded with 5- fluorouracil, a drug used to treat actinic keratosis and colon cancer, and producing a new Dermal Delivery System. The polymer-based (ethyl cellulose and eudragit RS 100) microsponge particles were prepared by the w/o/w double emulsification method. The optimized product was formed with the combination of independent variables levels: polymer (600 mg), stirring speed (1198 rpm) and surfactant (2% w/v), yielding responses as yield (~63.6257%), the average size of particles (~151.563 µm), entrapment efficiency (~75.319 %) and drug release in 8hr (~75.75%), with desirability value of 0.737. The products showed similar responses as obtained in scale-up work. FT-IR, DSC and SEM studies confirmed the drug's compatibility with polymers and porous morphology. Finally, gel embedded optimised product showed shear-thinning rheological property, ideal for drug release from the thixotropic gel.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

WITHDRAWN: Optimization and Scale-up Methodology in Preparing Microsponge Loaded with 5-Fluorouracil (5-FU).

Halder

Poddar²,

Khanam

2021

Preprint

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“…In addition, the regression equation showing the best fit using the selected mathematical models was used and validated by equating various statistical parameters such as p value, regular, adjusted and predicted correlation coefficient (r 2 ) [38,39]. Polynomial equations generated 3-dimensional surface and contour graphs were produced by the software.…”

Section: Experimental Design Tool (Design Expert ® )mentioning

confidence: 99%

Luteolin-Loaded Elastic Liposomes for Transdermal Delivery to Control Breast Cancer: In Vitro and Ex Vivo Evaluations

et al. 2021

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The study aimed to prepare and optimize luteolin (LUT)-loaded transdermal elastic liposomes (LEL1-LEL12), followed by in vitro and ex vivo evaluations of their ability to control breast cancer. Various surfactants (Span 60, Span 80, and Brij 35), and phosphatidyl choline (PC) as a lipid, were used to tailor various formulation as dictated by “Design Expert® software (DOE). These were characterized for size, polydispersity index (PDI), and zeta potential. The optimized formulation (OLEL1) was selected for comparative investigations (in vitro and ex vivo) against lipo (conventional liposomes) and drug suspension (DS). Moreover, the in vitro anticancer activity of OLEL1 was compared against a control using MCF-7 cell lines. Preliminary selection of the suitable PC: surfactant ratio for formulations F1–F9 showed relative advantages of Span 80. DOE suggested two block factorial designs with four center points to identify the design space and significant factors. OLEL1 was the most robust with high functional desirability (0.95), minimum size (202 nm), relatively high drug release, increased drug entrapment (92%), and improved permeation rate (~3270 µg/cm2) as compared with liposomes (~1536 µg/cm2) over 24 h. OLEL1 exhibited a 6.2- to 2.9-fold increase in permeation rate as compared with DS (drug solution). The permeation flux values of OLEL1, and lipo were found to be 136.3, 64 and 24.3 µg/h/cm2, respectively. The drug disposition values were 670 µg, 473 µg and 148 µg, for OLEL1, lipo and DS, respectively. Thus, ex vivo parameters were significantly better for OLEL1 compared with lipo and DS which is attributed to the flexibility and deformability of the optimized formulation. Furthermore, OLEL1 was evaluated for anticancer activity and showed maximized inhibition as compared with DS. Thus, elastic liposomes may be a promising approach for improved transdermal delivery of luteolin, as well as enhancing its therapeutic efficacy in controlling breast cancer.

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“…Spreadabilty is another rheological parameter based on "slip" and "drag" characteristics of the optimized n-HPTF-06 by using a modi ed spreadability apparatus [34]. Brie y, 1 gm of the optimized n-HPTF-06 was placed (in a sandwich form) on glass plate (upper) having measurement (L×B) 10×4 cm was xed with another glass plate (below) with same measurement and a graph paper embedded below it.…”

Section: Spreadabilitymentioning

confidence: 99%

Design and Optimization of a Novel-Herbosomal Loaded PEG-Poloxamer Topical Formulation For the Treatment of Cold Injuries: A Quality By Design Approach

Yadav

Pathak

Varshney

et al. 2021

Preprint

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Cold injury/injuries can range from minor chilblain to extreme form of frostbite. Cold injuries are pathologically a combination of ice crystal formation in tissue with inflammation, thrombosis and ischemia to extremities, necessitating limb amputation in extreme cases due to tissue necrosis. Less severe forms of cold injuries can be managed by gentle rewarming of limb and avoiding exposure to cold leading to favorable outcomes, however severe forms of frostbite are a cause of major concern to patients as well as the treating physician. Due to lack of effective pre-treatment modalities and paucity of research in prophylaxis and therapeutics of cold injuries, we have developed a novel-herbosomal loaded PEG-Poloxamer topical formulation (n-HPTF) by Quality by Designed approach, incorporating natural ingredients which are having potential therapeutic effect for the treatment of cold injury in a form of a novel-lipid vesicles (herbosomes) loaded in polymers (PEG-3350 and Poloxamer-188) resulting excellent occlusive barrier and thus promote rapid healing. Optimized novel-herbosomes showed entrapment efficiency > 90% and < 300 nm mean particle size and in-vitro drug permeation of about 2 µg/cm2 followed by Higuchi’s release kinetic. Skin irritancy study on female Sprague Dawley rats showed no edema or erythema. In-vivo bio-efficacy study was performed and found significantly good at p-value < 0.05 when compared to the standard treatment groups.

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Formulation and optimization of microsponge-loaded emulgel to improve the transdermal application of acyclovir—a DOE based approach

Cited by 29 publications

References 33 publications

WITHDRAWN: Optimization and Scale-up Methodology in Preparing Microsponge Loaded with 5-Fluorouracil (5-FU).

WITHDRAWN: Optimization and Scale-up Methodology in Preparing Microsponge Loaded with 5-Fluorouracil (5-FU).

Luteolin-Loaded Elastic Liposomes for Transdermal Delivery to Control Breast Cancer: In Vitro and Ex Vivo Evaluations

Design and Optimization of a Novel-Herbosomal Loaded PEG-Poloxamer Topical Formulation For the Treatment of Cold Injuries: A Quality By Design Approach

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