Synthesis of Tilmicosin Nanostructured Lipid Carriers for Improved Oral Delivery in Broilers: Physiochemical Characterization and Cellular Permeation

Sahito, Benazir; Zhang, Qian; Yang, Haifeng; Lin, Peng; Gao, Xiaona; Kashif, Jam; Aabdin, Zainul; Jiang, Shanxiang; Wang, Liping; Guo, Dawei

doi:10.3390/molecules25020315

Cited by 7 publications

(9 citation statements)

References 35 publications

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“…The absorption bands between 1100 and 1200 cm −1 were from ether and cyclic C‐C bonds in the ring structure of pectin molecules. For Til, the principal vibration absorption peaks are: O‐H at 3440 cm −1 , C‐H at 2940 cm −1 , C=O at 1750 cm −1 and 1690 cm −1 , C=C at 1580 cm −1 and C‐O at 1050 cm −1 29 . The presence of many components with O‐H functions could be the factor that increments the signal at 3250–3750 cm −1 in particles studies 2 .…”

Section: Resultsmentioning

confidence: 98%

Modulating drug release from poly(lactic‐co‐glycolic) acid microparticles by the addition of alginate and pectin

Karp

Satler

Busatto

et al. 2020

J of Applied Polymer Sci

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The aim of the present work is the characterization of PLGA microparticles including biopolymers for the controlled release of tilmicosin, a broad‐spectrum antibiotic. Microparticles were prepared using the double‐emulsion solvent evaporation technique. The effect of alginate and pectin incorporation over particle size and porosity, encapsulation efficiency (EE) and pH‐responsive drug release was evaluated. Formulations presented a mean particle size of 5.5 μm approximately and a drug EE ranged from 22%–57%. PLGA‐Alginate particles showed an increased porosity. Tilmicosin release profiles from PLGA and PLGA‐biopolymer microparticles were affected by the particular combination of polymers and the pH of the release medium. The experimental data was simulated using a mathematical model, which takes into account the autocatalytic polymer degradation and the different mechanisms of drug transport. The combination of PLGA and biopolymers strongly influenced the morphology of the particles, offering the possibility of controlling the drug release profiles according to the therapy.

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Section: Resultsmentioning

confidence: 98%

Modulating drug release from poly(lactic‐co‐glycolic) acid microparticles by the addition of alginate and pectin

Karp

Satler

Busatto

et al. 2020

J of Applied Polymer Sci

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“… 24 In addition, TIM-loaded lipid nanocarriers prepared through the high shear method display excellent storage and gastrointestinal stability and consequently enhanced oral absorption in broilers. 3 , 4 Zhou et al found that TIM-loaded in alginate-chitosan nanogels shows stronger sustained drug release compared with the injection of pure TIM. 5 Although previous studies have achieved the successful encapsulation and protection of TIM, facile preparation of TIM-loaded polymeric NPs with well-controlled size and tunable properties and functions remains a challenge.…”

Section: Introductionmentioning

confidence: 99%

Facile Preparation of Tilmicosin-Loaded Polymeric Nanoparticle with Controlled Properties and Functions

Wang

Bhutto

et al. 2020

ACS Omega

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As one of the effective broad-spectrum antimicrobial and anti-inflammatory drugs, tilmicosin (TIM) is applied extensively in a wide range of veterinary treatments. However, the low bioavailability typically leads to overuse of TIM in practical applications, which can cause residual accumulation in the environment and contamination of foodstuffs. Here, we report a precipitation method that allows us to prepare TIM-loaded poly(methyl methacrylate- co -methacrylic acid) (P(MMA- co -MAA)) nanoparticles. Specifically, TIM and biocompatible P(MMA- co -MAA) are dissolved in methanol and then water is introduced as an antisolvent, which triggers the co-precipitation and leads to well-controlled nanoparticles. Depending on the drug/polymer mass ratio and the total concentration of drug and polymer, the formed nanoparticles display a tunable radius from 27 to 80 nm with a narrow size distribution, a high drug loading content, and a controlled release of TIM. The encapsulation does not interrupt the antibacterial function of TIM while reducing its cytotoxicity enormously. Moreover, the formed nanoparticles could be dried to powder through freeze-drying, and the redispersion of the particles hardly disturbs the particle size, size distribution, and drug loading content. Our study developed a facile and robust precipitation method for the controlled construction of TIM-loaded polymeric nanoparticles with tunable properties and functions, as well as improved biocompatibility, which shall improve the bioavailability of TIM and enhance the practical applications.

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“…Sahito et al, also fabricated three types of tilmicosin-loaded NLCs to enhance the oral bioavailability of the drug [ 175 ]. NLCs were prepared by high shear and ultrasonic methods with palmitic acid, lauric acid, or stearic acid as a solid lipid, oleic acid as oil, and Tween 20 as a surfactant.…”

Section: Recently Developed Formulations To Bypass P-gp and Enhance Oral Bioavailability Of P-gp Substratesmentioning

confidence: 99%

Pharmaceutical Formulations with P-Glycoprotein Inhibitory Effect as Promising Approaches for Enhancing Oral Drug Absorption and Bioavailability

2021

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P-glycoprotein (P-gp) is crucial in the active transport of various substrates with diverse structures out of cells, resulting in poor intestinal permeation and limited bioavailability following oral administration. P-gp inhibitors, including small molecule drugs, natural constituents, and pharmaceutically inert excipients, have been exploited to overcome P-gp efflux and enhance the oral absorption and bioavailability of many P-gp substrates. The co-administration of small molecule P-gp inhibitors with P-gp substrates can result in drug–drug interactions and increased side effects due to the pharmacological activity of these molecules. On the other hand, pharmaceutically inert excipients, including polymers, surfactants, and lipid-based excipients, are safe, pharmaceutically acceptable, and are not absorbed from the gut. Notably, they can be incorporated in pharmaceutical formulations to enhance drug solubility, absorption, and bioavailability due to the formulation itself and the P-gp inhibitory effects of the excipients. Different formulations with inherent P-gp inhibitory activity have been developed. These include micelles, emulsions, liposomes, solid lipid nanoparticles, polymeric nanoparticles, microspheres, dendrimers, and solid dispersions. They can bypass P-gp by different mechanisms related to their properties. In this review, we briefly introduce P-gp and P-gp inhibitors, and we extensively summarize the current development of oral drug delivery systems that can bypass and inhibit P-gp to improve the oral absorption and bioavailability of P-gp substrates. Since many drugs are limited by P-gp-mediated efflux, this review is helpful for designing suitable formulations of P-gp substrates to enhance their oral absorption and bioavailability.

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Synthesis of Tilmicosin Nanostructured Lipid Carriers for Improved Oral Delivery in Broilers: Physiochemical Characterization and Cellular Permeation

Cited by 7 publications

References 35 publications

Modulating drug release from poly(lactic‐co‐glycolic) acid microparticles by the addition of alginate and pectin

Modulating drug release from poly(lactic‐co‐glycolic) acid microparticles by the addition of alginate and pectin

Facile Preparation of Tilmicosin-Loaded Polymeric Nanoparticle with Controlled Properties and Functions

Pharmaceutical Formulations with P-Glycoprotein Inhibitory Effect as Promising Approaches for Enhancing Oral Drug Absorption and Bioavailability

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