Comparative study of cilnidipine loaded PLGA nanoparticles: process optimization by DoE, physico-chemical characterization and in vivo evaluation

Diwan, Rimpy; Khan, Shareef; Ravi, Punna Rao

doi:10.1007/s13346-020-00732-5

Cited by 12 publications

(9 citation statements)

References 34 publications

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“…The quadratic equation for both droplet size and % LE exhibited positive control of oil content on droplet size and negative control over % LE while in contrast to this increase in the extent of surfactant and cosurfactant paraded negative impact on droplet size and positive impact on % LE. The % LE dropped as the % of oil increased, possibly due to supersaturation of the internal phase, causing TRT release from the internal phase to the external phase during emulsification (Diwan et al, 2020). A low PDI score indicates a tapering particle size distribution and a consistent NE formulation.…”

Section: Discussionmentioning

confidence: 99%

“…At defined time intervals, for instance, 0, 0.25, 0.5, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 12, 18, and 24, aliquots of 1.5 ml sample were obtained, and fresh PBS was added to maintain the sink conditions. The samples were then tested using a UV spectrophotometer at 421 and 359 nm for CUR and TRT, respectively (Dhawan et al, 2014). The in vitro release study was repeated thrice to obtain accurate data.…”

Section: In-vitro Release Studymentioning

confidence: 99%

“…On the other hand, an increased amount of oil exhibited a substantial negative influence on the % LE of TRT in TRT-CUR-NE during emulsification, as shown in Figure 1 and Equation (4). The % LE dropped as the % of oil increased, possibly due to supersaturation of the internal phase, causing TRT release from the internal phase to the external phase during emulsification (Diwan et al, 2020).…”

Section: Effect Of Critical Factors On % Le (Y 2 )mentioning

confidence: 99%

“…The amount of surfactant and co-surfactant had a negative impact on particle size, as the particle size decreased upon increasing the amount of surfactant and cosurfactant(Yeo et al, 2021).On the other hand, an increased amount of oil exhibited a substantial negative influence on the % LE of TRT in TRT-CUR-NE during emulsification, as shown in Figure1and Equation (4). The % LE dropped as the % of oil increased, possibly due to supersaturation of the internal phase, causing TRT release from the internal phase to the external phase during emulsification(Diwan et al, 2020).…”

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confidence: 99%

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A co-additive nanoemulgel formulation of tretinoin and curcumin: Formulation and optimization

Phaugat¹,

Nishal²,

Dutt³

et al. 2022

j app pharm sci

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Tretinoin (TRT), a natural all-trans retinoic acid occurring retinoid metabolite, belongs to the first generation of retinoids used to treat various skin ailments, like acne vulgaris and skin ageing and psoriasis. In this study, a combination of drugs using TRT and curcumin (CUR) nanoemulsion (NE) is fabricated, and is further added to a gel formulation to boost the efficacy and stability of the topical formulation. A high-energy sonication technique was used in the NE fabrication, and optimization was carried out using the Box-Behnken design. The TRT-CUR-NEs were found to have a mean particle size, zeta potential, and PDI of 77.6 ± 2.1 nm, −20.7 ± 4.4 mV, and 0.268 ± 0.029, respectively. The optimized formulation of TRT-CUR-NE has a % entrapment efficiency of 85.92% ± 2.6% and 88.31% ± 3.2% for TRT and CUR, respectively, and a % loading efficiency of 19.6% ± 1.2% and 18.7% ± 2.5%, respectively, for TRT and CUR, respectively. The in vitro release profile displayed % cumulative drug release of 28.64% ± 0.31%, 80.32% ± 0.42%, and 89.64% ± 0.97% after 24 hours for plain gel, TRT-CUR-NE, and TRT-CUR-nanoemulgel, respectively.

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Section: Discussionmentioning

confidence: 99%

Section: In-vitro Release Studymentioning

confidence: 99%

Section: Effect Of Critical Factors On % Le (Y 2 )mentioning

confidence: 99%

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confidence: 99%

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A co-additive nanoemulgel formulation of tretinoin and curcumin: Formulation and optimization

Phaugat¹,

Nishal²,

Dutt³

et al. 2022

j app pharm sci

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“…Drugs in BCS Classes II (low solubility, high permeability), III (high solubility, low permeability) and IV (low solubility, low permeability) show low bioavailability when orally administered. Therefore, in the process of formulation, efforts have been made to improve bioavailability by various techniques such as particle size reduction, lipid-based formulations, solid dispersions, and absorption enhancers [ 10 – 14 ].…”

Section: Introductionmentioning

confidence: 99%

Nano-hydroxyapatite improves intestinal absorption of acetazolamide (BCS Class IV drug)–but how?

2022

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We earlier reported that coating poorly water-soluble drugs with nano-hydroxyapatite (nano-HAP) improves bioavailability after oral administration. In the present study, we coated BCS Class IV drug acetazolamide (AZ) with nano-HAP (AZ/HAP formulation), and investigated its bioavailability and nano-HAP’s role in promoting it. We tested AZ bioavailability after a single oral dose of the AZ/HAP formulation in rats, followed by a series of in vitro, ex vivo and in vivo testing. The binding state of AZ and nano-HAP was analyzed by gel filtration chromatography. AZ permeability was studied using a Caco-2 cell monolayer assay kit, to test for tight junction penetration, then using an Ussing chamber mounted with intestinal epithelium, both with and without Peyer’s patch tissue, to examine the role of intracellular transport. Fluorescence-labeled nano-HAP particles were administered orally in rats to investigate their localization in the intestinal tract. The area under the blood concentration time-curve in rats was about 4 times higher in the AZ/HAP formulation group than in the untreated AZ group. Gel filtration analysis showed AZ and nano-HAP were not bound. The Caco-2 study showed equivalent AZ permeability for both groups, but without significant change in transepithelial electrical resistance (TEER), indicating that tight junctions were not penetrated. In the Ussing chamber study, no significant difference in AZ permeability between the two groups was observed for epithelium containing Peyer’s patch tissue, but for epithelium without Peyer’s patch tissue, at high concentration, significantly higher permeability in the AZ/HAP formulation group was observed. Fluorescent labeling showed nano-HAP particles were present in both intestinal villi and Peyer’s patch tissue 30 min after oral administration. Our results suggest that nano-HAP’s enhancement of drug permeability from the small intestine occurs not via tight junctions, but intracellularly, via the intestinal villi. Further study to elucidate the mechanism of this permeability enhancement is required.

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Polyester nanoparticles delivering chemotherapeutics: Learning from the past and looking to the future to enhance their clinical impact in tumor therapy

Longobardi,

Moore,

Conte

et al. 2024

WIREs Nanomed Nanobiotechnol

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Polymeric nanoparticles (NPs), specifically those comprised of biodegradable and biocompatible polyesters, have been heralded as a game‐changing drug delivery platform. In fact, poly(α‐hydroxy acids) such as polylactide (PLA), poly(lactide‐co‐glycolide) (PLGA), and poly(ε‐caprolactone) (PCL) have been heavily researched in the past three decades as the material basis of polymeric NPs for drug delivery applications. As materials, these polymers have found success in resorbable sutures, biodegradable implants, and even monolithic, biodegradable platforms for sustained release of therapeutics (e.g., proteins and small molecules) and diagnostics. Few fields have gained more attention in drug delivery through polymeric NPs than cancer therapy. However, the clinical translational of polymeric nanomedicines for treating solid tumors has not been congruent with the fervor or funding in this particular field of research. Here, we attempt to provide a comprehensive snapshot of polyester NPs in the context of chemotherapeutic delivery. This includes a preliminary exploration of the polymeric nanomedicine in the cancer research space. We examine the various processes for producing polyester NPs, including methods for surface‐functionalization, and related challenges. After a detailed overview of the multiple factors involved with the delivery of NPs to solid tumors, the crosstalk between particle design and interactions with biological systems is discussed. Finally, we report state‐of‐the‐art approaches toward effective delivery of NPs to tumors, aiming at identifying new research areas and re‐evaluating the reasons why some research avenues have underdelivered. We hope our effort will contribute to a better understanding of the gap to fill and delineate the future research work needed to bring polyester‐based NPs closer to clinical application.This article is categorized under: Therapeutic Approaches and Drug Discovery > Nanomedicine for Oncologic Disease Nanotechnology Approaches to Biology > Nanoscale Systems in Biology Therapeutic Approaches and Drug Discovery > Emerging Technologies

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Comparative study of cilnidipine loaded PLGA nanoparticles: process optimization by DoE, physico-chemical characterization and in vivo evaluation

Cited by 12 publications

References 34 publications

A co-additive nanoemulgel formulation of tretinoin and curcumin: Formulation and optimization

A co-additive nanoemulgel formulation of tretinoin and curcumin: Formulation and optimization

Nano-hydroxyapatite improves intestinal absorption of acetazolamide (BCS Class IV drug)–but how?

Polyester nanoparticles delivering chemotherapeutics: Learning from the past and looking to the future to enhance their clinical impact in tumor therapy

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