Formulation and Evaluation of Cefixime Nanosuspension for the Enhancement of Oral Bioavailability by Solvent-Antisolvent Method and its Suitable Method Development

Mastiholimath, Vinayak Shivamurthi; Rajendra, Bhagat Ankita; Mannur, V. S.; Dandagi, Panchaxari Mallappa; Gadad, Anand Panchakshari; Khanal, Pukar

doi:10.5530/ijper.54.1.7

Cited by 6 publications

(3 citation statements)

References 21 publications

(39 reference statements)

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“…Further, the formulation was transferred to an amber-colored bottle and stored in the refrigerator. 8…”

Section: Methods Of Preparation Of Darifenacine Hbr Nanosuspensionmentioning

confidence: 99%

Preparation and In-vitro Evaluation of Darifenacin HBr as Nanoparticles Prepared as Nanosuspension

Al-Obaidy¹,

Rajab²

2022

IJDDT

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Nanosuspension is a term that can be used to describe a colloidal dispersion of nanosized droplets of the drug in an aqueous medium with a size below 1 μm. Drug nanoparticles are one of the most significant methods to reduce the constituent part diameter and increase surface area, improving the dissolution and oral bioavailability of hydrophobic medicines, enhancing drug dissolution rate and bioavailability. Nanoparticles are produced using appropriate techniques for drug delivery applications and administered via various routes, including oral, topical, parenteral, ophthalmic, and pulmonary. Overactive bladder (OAB) affects around 16% of adults and is more common as people become older. It causes a variety of symptoms, including urgency, incontinence, urine frequency, and nocturia. DH. It is newly drug used to treat complicated OAB. It has a higher selectivity for the bladder’s muscarinic receptors. After intravenous and immediate-release oral dose forms. It suffers from extensive first-pass metabolism with a short elimination half-life and ranging between three to four hours). The current research focused on creating an extended-release dosage form utilizing Eudragit RS100. The solvent/anti-solvent precipitation method was used to make darifenacine nanoparticles. A certain quantity of medication was dissolved in a water-miscible solvent (methanol), then poured at a specific speed into water containing stabilizer on a magnetic stirrer for a 1/2-hour; after that, the resulted product was sonicated at 37°C for 15 minutes. The physicochemical interaction among medication with additives was explored utilizing fourier transform infrared spectroscopy (FTIR) and differential scanning calorimetric (DSC). The particle size and zeta potential of the generated nanosuspension were calculated.

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“…Further, the formulation was transferred to an amber-colored bottle and stored in the refrigerator. 8…”

Section: Methods Of Preparation Of Darifenacine Hbr Nanosuspensionmentioning

confidence: 99%

Preparation and In-vitro Evaluation of Darifenacin HBr as Nanoparticles Prepared as Nanosuspension

Al-Obaidy¹,

Rajab²

2022

IJDDT

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“…Nanosuspensi adalah salah satu bentuk sediaan berbasis nanoteknologi (5). Nanosuspensi merupakan sistem dispersi koloidal mengandung partikel obat dengan ukuran <1µm yang distabilkan oleh surfaktan dan atau polimer (6).…”

Section: Pendahuluanunclassified

Kajian Pengembangan Sediaan Nanosuspensi Untuk Penghantaran Intravena Obat Sukar Larut Air

Priani

2022

Maj. Farmasetika

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Pengembangan bentuk sediaan perlu dilakukan untuk penghantaran intravena senyawa aktif dengan kelarutan yang rendah dalam air. Nanosuspensi sebagai suatu produk nanoteknologi banyak diaplikasikan untuk tujuan tersebut. Penelitian ini bertujuan untuk mengkaji pengembangan sistem nanosuspensi untuk penghantaran intravena obat sukar larut air dalam hal jenis penstabil yang aman digunakan dan mengkaji pengaruhnya terhadap disolusi, pelepasan , dan profil farmakokinetika zat aktif serta kajian keamanan penggunaan. Penelitian dilakukan dengan systematic literature review (SLR), menggunakan artikel ilmiah dari database bereputasi yang memenuhi kriteria inklusi dan eksklusi yang sudah ditetapkan. Hasil kajian menunjukkan bahan penstabil utama yang digunakan pada pengembangan nanosuspensi intravena adalah poloxamer, lesitin, TPGS (D-a-tocopheryl polyethylene glycol 1000 succinate), dan BSA (bovine serum albumin) yang bersifat biokompatibel, non toksik, dengan harus memperhatikan kadar maksimal menurut FDA’s Inactive Ingredient Database for IV route. Pengembangan nanosuspensi secara signifikan mampu meningkatkan disolusi dan pelepasan zat aktif dibandingkan dengan bentuk murni/suspensi. Pengembangan nanosuspensi pada beberapa bahan aktif mampu merubah profil farmakokinetika yang ditandai dengan peningkatan nilai AUC (area under curve), Cmax, dan MRT (mean residence time) dengan memberikan profil pelepasan diperlambat (sustained release). Pengembangan nanosuspensi pada beberapa bahan aktif terbukti aman digunakan secara intravena berdasarkan uji hemolisis dan iritasi vaskular. Berdasarkan kajian yang telah dilakukan diketahui bahwa nanosuspensi sesuai dan potensial untuk diaplikasikan untuk penghantaran intravena obat sukar larut air.

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“…However, as per the biopharmaceutical classification system (BCS), CFX belongs to class IV drugs, exhibiting poor water solubility and less permeability across the absorption membrane when given orally [ 7 ]. The oral bioavailability of CFX reported in the literature ranged from 30 to 50% only, with the lower range for solid dosage forms such as tablets and the higher range for liquids such as solutions [ 8 ]. Therefore, high doses are often required, especially in cases of Staphylococcus aureus infections, to achieve the therapeutics outcomes and minimize the chances of resistance.…”

Section: Introductionmentioning

confidence: 99%

Enhanced Intestinal Permeability of Cefixime by Self-Emulsifying Drug Delivery System: In-Vitro and Ex-Vivo Characterization

et al. 2023

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Background: Cefixime (CFX) belongs to a group of third-generation cephalosporin antibiotics with low water solubility and low intestinal permeability, which ultimately leads to significantly low bioavailability. Aim: This study aimed to increase solubility, improve drug release, and intestinal permeability of CFX by loading into SEDDS. Methods: Suitable excipients were selected based on drug solubility, percent transmittance, and emulsification efficiency. Pseudo-ternary phase diagram was fabricated for the identification of effective self-emulsification region. The best probably optimized formulations were further assessed for encumbered drug contents, emulsification time, cloud point measurement, robustness to dilution, mean droplet size, zeta potential, polydispersity index (PDI), and thermodynamic and chemical stability. Moreover, in vitro drug release studies and ex vivo permeation studies were carried out and apparent drug permeability Papp of different formulations was compared with the marketed brands of CFX. Results: Amongst the four tested SEDDS formulations, F-2 formulation exhibited the highest drug loading of 96.32%, emulsification time of 40.37 ± 3 s, mean droplet size of 19.01 ± 1.12 nm, and demonstrated improved long-term thermodynamic and chemical stability when stored at 4 °C. Release studies revealed a drug release of 97.32 ± 4.82% within 60 min in simulated gastric fluid. Similarly, 97.12 ± 5.02% release of CFX was observed in simulated intestinal fluid within 120 min; however, 85.13 ± 3.23% release of CFX was observed from the marketed product. Ex vivo permeation studies displayed a 2.7-fold increase apparent permeability compared to the marketed product in 5 h. Conclusion: Owing to the significantly improved drug solubility, in vitro release and better antibacterial activity, it can be assumed that CFX-loaded SEDDS might lead to an increased bioavailability and antibacterial activity, possibly leading to improved therapeutic effectiveness.

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Formulation and Evaluation of Cefixime Nanosuspension for the Enhancement of Oral Bioavailability by Solvent-Antisolvent Method and its Suitable Method Development

Cited by 6 publications

References 21 publications

Preparation and In-vitro Evaluation of Darifenacin HBr as Nanoparticles Prepared as Nanosuspension

Preparation and In-vitro Evaluation of Darifenacin HBr as Nanoparticles Prepared as Nanosuspension

Kajian Pengembangan Sediaan Nanosuspensi Untuk Penghantaran Intravena Obat Sukar Larut Air

Enhanced Intestinal Permeability of Cefixime by Self-Emulsifying Drug Delivery System: In-Vitro and Ex-Vivo Characterization

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