Systematically optimized biocompatible isotretinoin-loaded solid lipid nanoparticles (SLNs) for topical treatment of acne

Raza, Kaisar; Singh, Bhupinder; Singal, Parteek; Wadhwa, Sheetu; Katare, Om Prakash

doi:10.1016/j.colsurfb.2012.12.043

Cited by 114 publications

(47 citation statements)

References 25 publications

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“…Bragagni made use of the elements of the concept the research on niosomes [28]. The investigations by Raza et al revealed the importance of systematic optimization of the development of solid-lipid nanoparticles [29], and Verma et al…”

Section: Qbd In Pharmaceutical Nano-developmentmentioning

confidence: 99%

Adaptation of the quality by design concept in early pharmaceutical development of an intranasal nanosized formulation

Pallagi

Ambrus

Szabó‐Révész

et al. 2015

International Journal of Pharmaceutics

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Section: Qbd In Pharmaceutical Nano-developmentmentioning

confidence: 99%

Adaptation of the quality by design concept in early pharmaceutical development of an intranasal nanosized formulation

Pallagi

Ambrus

Szabó‐Révész

et al. 2015

International Journal of Pharmaceutics

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“…The rat skin was clamped between the donor and the receptor chambers of modified Franz diffusion cells (area ¼ 0.95 cm 2 ), where the stratum corneum side faced the donor compartment and the dermal side faced the receptor compartment. The receptor compartment was filled with 10 mL 50% v/v ethanoic phosphate buffer saline (pH 7.4) to maintain sink conditions for agomelatine (saturated solubility ¼ 0.5 mg/mL) (Magnusson & Koskinen, 2000;Raza et al, 2013b). The receptor chambers were thermostatically heated to 37 ± 0.5 C and their content was magnetically stirred at 100 rpm through the whole experiment time.…”

Section: Ex Vivo Permeationmentioning

confidence: 99%

Transdermal agomelatine microemulsion gel: pyramidal screening, statistical optimization and in vivo bioavailability

et al. 2017

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Agomelatine is a new antidepressant having very low oral drug bioavailability less than 5% due to being liable to extensive hepatic 1st pass effect. This study aimed to deliver agomelatine by transdermal route through formulation and optimization of microemulsion gel. Pyramidal screening was performed to select the most suitable ingredients combinations and then, the design expert software was utilized to optimize the microemulsion formulations. The independent variables of the employed mixture design were the percentages of capryol 90 as an oily phase (X 1 ), Cremophor RH40 and Transcutol HP in a ratio of (1:2) as surfactant/cosurfactant mixture 'S mix ' (X 2 ) and water (X 3 ). The dependent variables were globule size, optical clarity, cumulative amount permeated after 1 and 24 h, respectively (Q1 and Q 24 ) and enhancement ratio (ER). The optimized formula was composed of 5% oil, 45% S mix and 50% water. The optimized microemulsion formula was converted into carbopol-based gel to improve its retention on the skin. It enhanced the drug permeation through rat skin with an enhancement ratio of 37.30 when compared to the drug hydrogel. The optimum ME gel formula was found to have significantly higher C max , AUC 0-24 h and AUC 0-1 than that of the reference agomelatine hydrogel and oral solution. This could reveal the prosperity of the optimized microemulsion gel formula to augment the transdermal bioavailability of agomelatine. ARTICLE HISTORY

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“…The mean value of three repeated measurements for each sample was reported as the final measurement. SLN sample was diluted with sufficient water, a diluted sample was directly placed into a cuvette, and mean particle size and polydispersibility index were measured [18][19][20]. Zeta potential measurement was carried out with the same instrument Zetasizer Nano ZS.…”

Section: Micromeritics Measurementmentioning

confidence: 99%

Continuous Production of Fenofibrate Solid Lipid Nanoparticles by Hot-Melt Extrusion Technology: a Systematic Study Based on a Quality by Design Approach

Patil

Feng

et al. 2014

AAPS J

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Abstract. This contribution describes a continuous process for the production of solid lipid nanoparticles (SLN) as drug-carrier systems via hot-melt extrusion (HME). Presently, HME technology has not been used for the manufacturing of SLN. Generally, SLN are prepared as a batch process, which is time consuming and may result in variability of end-product quality attributes. In this study, using Quality by Design (QbD) principles, we were able to achieve continuous production of SLN by combining two processes: HME technology for melt-emulsification and high-pressure homogenization (HPH) for size reduction. Fenofibrate (FBT), a poorly water-soluble model drug, was incorporated into SLN using HME-HPH methods. The developed novel platform demonstrated better process control and size reduction compared to the conventional process of hot homogenization (batch process). Varying the process parameters enabled the production of SLN below 200 nm. The dissolution profile of the FBT SLN prepared by the novel HME-HPH method was faster than that of the crude FBT and a micronized marketed FBT formulation. At the end of a 5-h in vitro dissolution study, a SLN formulation released 92-93% of drug, whereas drug release was approximately 65 and 45% for the marketed micronized formulation and crude drug, respectively. Also, pharmacokinetic study results demonstrated a statistical increase in Cmax, Tmax, and AUC 0-24 h in the rate of drug absorption from SLN formulations as compared to the crude drug and marketed micronized formulation. In summary, the present study demonstrated the potential use of hot-melt extrusion technology for continuous and large-scale production of SLN.

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Systematically optimized biocompatible isotretinoin-loaded solid lipid nanoparticles (SLNs) for topical treatment of acne

Cited by 114 publications

References 25 publications

Adaptation of the quality by design concept in early pharmaceutical development of an intranasal nanosized formulation

Adaptation of the quality by design concept in early pharmaceutical development of an intranasal nanosized formulation

Transdermal agomelatine microemulsion gel: pyramidal screening, statistical optimization and in vivo bioavailability

Continuous Production of Fenofibrate Solid Lipid Nanoparticles by Hot-Melt Extrusion Technology: a Systematic Study Based on a Quality by Design Approach

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