In vitro appraisals and ex vivo permeation prospect of chitosan nanoparticles designed for schizophrenia to intensify nasal delivery

Annu, .; Baboota, Sanjula; Ali, Javed

doi:10.1007/s00289-021-03598-w

Cited by 17 publications

(11 citation statements)

References 31 publications

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“…Annu et al have developed the chitosan nanoparticle. The result reported in the FT-IR study stated that the characteristic peaks of the drug in nanoparticles were absent compared to drug alone spectra, and it could be the possible reason for entrapment of the drug within the nanoformulation [ 52 ].…”

Section: Resultsmentioning

confidence: 99%

Ribociclib Nanostructured Lipid Carrier Aimed for Breast Cancer: Formulation Optimization, Attenuating In Vitro Specification, and In Vivo Scrutinization

Ali

Annu

Biswas

et al. 2022

BioMed Research International

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Purpose. The current investigation is on the explicit development and evaluation of nanostructured lipidic carriers (NLCs) through the oral route to overcome the inherent lacuna of chemotherapeutic drug, in which Ribociclib (RBO) was used for breast cancer to diminish the bioavailability issue. Method. The RBO-NLCs were prepared using the solvent evaporation method and optimized method by the Box–Behnken design (BBD). Various assessment parameters characterized the optimized formulation and their in vivo study. Results. The prepared NLCs exhibited mean particle size of 114.23 ± 2.75 nm , mean polydispersity index of 0.649 ± 0.043 , and high entrapment efficiency of 87.7 ± 1.79 % . The structural analysis by TEM revealed the spherical size of NLCs and uniform drug distribution. An in vitro drug release study was established through the 0.1 N HCl pH 1.2, acetate buffer pH 4.5, and phosphate buffer pH 6.8 with % cumulative drug release of 86.71 ± 8.14 , 85.82 ± 4.58 , and 70.98 ± 5.69 % , was found respectively, compared with the RBO suspension (RBO-SUS). In vitro intestinal gut permeation studies unveiled a 1.95-fold gain in gut permeation by RBO-NLCs compared with RBO-SUS. In vitro lipolysis suggests the drug availability at the absorption site. In vitro haemolysis study suggests the compatibility of NLCs to red blood cells compared to the suspension of the pure drug. The confocal study revealed the depth of penetration of the drug into the intestine by RBO-NLCs which was enhanced compared to RBO-SUS. A cell line study was done in MCF-7 and significantly reduced the IC50 value compared to the pure drug. The in vivo parameters suggested the enhanced bioavailability by 3.54 times of RBO-NLCs as compared to RBO-SUS. Conclusion. The in vitro, ex vivo, and in vivo results showed a prominent potential for bioavailability enhancement of RBO and effective breast cancer therapy.

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Section: Resultsmentioning

confidence: 99%

Ribociclib Nanostructured Lipid Carrier Aimed for Breast Cancer: Formulation Optimization, Attenuating In Vitro Specification, and In Vivo Scrutinization

Ali

Annu

Biswas

et al. 2022

BioMed Research International

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“…The chitosan-based nanoparticle was developed by Annu and associates, who stated that specific peaks of the drug, e.g., 3065 cm -1 (stretching of aromatic) and 3431 cm -1 (stretching of N-H), were absent in the nanoformulation when compared to the pure drug. It could be a probable reason for drug encapsulation within the polymer [46]. In addition, the peak at 265.201 °C coincided with the peak of ERVN; however, the intensity of the peak was relatively less due to the entrapment of the drug in the pores of the lipid matrix of LNCs, whereas the pure ERVN showed sharp peaks that represented the crystalline form of the drug.…”

Section: Structural Analysis By Ft-ir Spectroscopymentioning

confidence: 88%

“…The similarity values at various pH showed that the formulation, i.e., ERVN-TPGS-LNCs and the ERVN-S release pattern, were not matchable. Bellaiah and a coworker reported a similar comparison of ERVN-loaded solid lipid nanoparticle dissolution profiles or improvements in oral bioavailability [46,47]. The kinetic drug release models were computed in the various pH buffers (1.2, and 6.8).…”

Section: In-vitro Drug Releasementioning

confidence: 99%

Fabrication of TPGS decorated Etravirine loaded lipid nanocarriers as a neoteric oral bioavailability enhancer for lymphatic targeting

Muheem,

Wasim,

Aldosari

et al. 2023

Preprint

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Etravirine (ERVN) is a potential NNRTI (non-nucleoside reverse transcriptase inhibitor) in treating HIV infection. It possesses extremely low oral bioavailability. The present research aims to optimize the formulation and characterization of TPGS-enriched ERVN-loaded lipid-based nanocarriers (LNCs) for HIV-infected patients. The formulation, ERVN-TPGS-LNCs, was optimized by CCRD using a modified-solvent evaporation process. Various characterization parameters of LNCs were evaluated, including globule size of 121.56 ± 2.174 nm, PDI of 0.172 ± 0.042, the zeta potential of -7.32 ± 0.021 mV, %EE of 94.42 ± 8.65% of ETR and %DL was 8.94 ± 0.759% of ERVN and spherical shape was revealed by TEM. PXRD was also performed to identify the crystallinity of the sample. In-vitro drug release showed % a cumulative drug release of 79.77 ± 8.35% at pH 1.2 and 83.23 ± 9.11% at pH 6.8, respectively, at the end of 48h compared to pure drug suspension (ERVN-S). Further, the intestinal permeation study and confocal microscope showed approximately ~3-fold and ~2-fold increased permeation in ERVN-TPGS-LNCs and ERVN-LNCs across the gut sac compared to ERVN-S. Hemolysis compatibility and lipolysis studies were performed to predict the in-vivo fate of the formulation. The pharmacokinetic study revealed a 3.13-fold increment in the relative bioavailability, which agrees with the ex-vivo studies, and lymphatic uptake was validated by using cycloheximide (CYHD) along with designed formulation, which leads to lowering AUC of ERVN-TPGS-LNCs. Thus, this study ensures that ERVN-TPGS-LNCs take lymphatic uptake to minimize the first-pass metabolism followed by improved oral bioavailability of EVN. Thus, the enhanced bioavailability of ERVN can reduce the high dose of ERVN to minimize the adverse effects related to dose-related burden.

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“…Drug molecules including carboplatin, carmustine, diazepam, lorazepam, lurasidone, dolutegravir, and oxcarbazepine have been assessed by developing PNs for brain delivery by intranasal route [ 106 , 107 , 108 ]. Biodegradable and biocompatible polymers including chitosan, polycaprolactone, polylactic acid, and PLGA (poly lactic-co-glycolic acid), which are approved by the US FDA, were widely utilized in developing PNs aimed for intranasal delivery [ 109 ]. In one attempt, a direct nose-to brain delivery of lamotrigine-loaded PLGA PNs was assessed in rats for effective therapy in neuropathic pain [ 110 ].…”

Section: Nanoparticles For Nose-to-brain Drug Deliverymentioning

confidence: 99%

Nasal Delivery to the Brain: Harnessing Nanoparticles for Effective Drug Transport

Gandhi,

Shastri,

Shah

et al. 2024

Pharmaceutics

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The nose-to-brain drug-delivery system has emerged as a promising strategy to overcome the challenges associated with conventional drug administration for central nervous system disorders. This emerging field is driven by the anatomical advantages of the nasal route, enabling the direct transport of drugs from the nasal cavity to the brain, thereby circumventing the blood–brain barrier. This review highlights the significance of the anatomical features of the nasal cavity, emphasizing its high permeability and rich blood supply that facilitate rapid drug absorption and onset of action, rendering it a promising domain for neurological therapeutics. Exploring recent developments and innovations in different nanocarriers such as liposomes, polymeric nanoparticles, solid lipid nanoparticles, dendrimers, micelles, nanoemulsions, nanosuspensions, carbon nanotubes, mesoporous silica nanoparticles, and nanogels unveils their diverse functions in improving drug-delivery efficiency and targeting specificity within this system. To minimize the potential risk of nanoparticle-induced toxicity in the nasal mucosa, this article also delves into the latest advancements in the formulation strategies commonly involving surface modifications, incorporating cutting-edge materials, the adjustment of particle properties, and the development of novel formulations to improve drug stability, release kinetics, and targeting specificity. These approaches aim to enhance drug absorption while minimizing adverse effects. These strategies hold the potential to catalyze the advancement of safer and more efficient nose-to-brain drug-delivery systems, consequently revolutionizing treatments for neurological disorders. This review provides a valuable resource for researchers, clinicians, and pharmaceutical-industry professionals seeking to advance the development of effective and safe therapies for central nervous system disorders.

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In vitro appraisals and ex vivo permeation prospect of chitosan nanoparticles designed for schizophrenia to intensify nasal delivery

Cited by 17 publications

References 31 publications

Ribociclib Nanostructured Lipid Carrier Aimed for Breast Cancer: Formulation Optimization, Attenuating In Vitro Specification, and In Vivo Scrutinization

Ribociclib Nanostructured Lipid Carrier Aimed for Breast Cancer: Formulation Optimization, Attenuating In Vitro Specification, and In Vivo Scrutinization

Fabrication of TPGS decorated Etravirine loaded lipid nanocarriers as a neoteric oral bioavailability enhancer for lymphatic targeting

Nasal Delivery to the Brain: Harnessing Nanoparticles for Effective Drug Transport

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