A key role by polymers in microneedle technology: a new era

The dose frequency of drugs belonging to class II is usually high and associated with harmful effects on the body. The study aimed to enhance the solubility of the poorly water-soluble drug amoxicillin (AM) by the solid dispersion (SD) technique. Six different SDs of AM, F1−F6, were prepared by the spray drying technique using two other carriers, HP-β-CD (F1−F3) and HPMC (F4−F6), in 1:1, 1:2, and 1:3 drug-to-polymer ratios. These SDs were analyzed to determine their practical yield, drug content, and aqueous solubility using analytical techniques such as Fourier transform infrared spectroscopy, scanning electron microscopy, thermogravimetric analysis, and powder X-ray diffraction. The effect of polymer concentration on SDs was determined using aqueous solubility, in vitro dissolution, and in vivo studies. The results showed no drug−polymer interactions in SDs. Solubility studies showed that SDs based on the drug-to-polymer ratio of 1:2 (F2 and F5) were highly soluble in water compared to those with ratios of 1:1 and 1:3. In vitro dissolution studies also showed that SDs with a ratio of 1:2 released the highest drug concentration from both polymeric systems. The SDs based on HPMC confirmed the more sustained release of the drug as compared to that of HP-β-CD. All the SDs were observed as stable and amorphous, with a smooth spherical surface. In vivo studies reveal the enhancement of pharmacokinetics parameters as compared to standard AM. Hence, it is confirmed that spray drying is an excellent technique to enhance the solubility of AM in an aqueous medium. This may contribute to the enhancement of the pharmacokinetic behaviors of SDs.

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“…Consequently, the diffusional path length is also lengthened. This leads to a reduction in the solubility rate …”

Section: Resultsmentioning

confidence: 99%

Pharmaceutical and Pharmacological Evaluation of Amoxicillin after Solubility Enhancement Using the Spray Drying Technique

et al. 2022

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“…Polypyrroles (PPy) are one of the most intensively studied conducting polymers due to their simple and inexpensive preparation, along with their widely admitted character as good sensors, actuators, and solar cell materials. , Conducting polymers are characterized by alternate double and single bonds and have tremendous applications in interdisciplinary science . Since neutral polypyrrole has a broadband gap and makes it difficult to move electrons from the valence band to the conduction band, it is considered to be an insulator.…”

Section: Introductionmentioning

confidence: 99%

Polaron Formation in Conducting Polymers: A Novel Approach to Designing Materials with a Larger NLO Response

Ahsin,

Ejaz,

Sarfaraz

et al. 2024

ACS Omega

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Substantial efforts have been made to design and investigate new approaches for high-performance nonlinear optical (NLO) materials. Herein, we report polaron formation in conducting polymers as a new approach to designing materials with a large NLO response. A comparative study of polypyrrole and polypyrrole-based polaron (nPy + where n = 1, 3, 5, 7, and 9) is carried out for optoelectronic and NLO properties. The studied polarons (PPy + ) show excellent electronic properties and have reduced ionization potential (IP) as compared to neutral PPy, and a monotonic decrease is observed with increased chain lengths (1Py to 9Py). Interesting trends of global reactivity descriptors can be seen; the softness (S) increases with an increase in the chain length of PPy, while the hardness (η) decreases in the same fashion. The E H-L gaps for the PPy + polaronic state are significantly lower than their corresponding neutral PPy. In the polaronic model (PPy + ), radicals decisively reduce the crucial excitation energy, reminiscent of excess electrons (alkali metals). The performed TDOS spectral analysis further justifies the better conductive and electronic properties of polarons (PPy + ) with increased chain lengths (conjugation). The static hyperpolarizability response (β o ) is recorded up to 1.3 × 10 2 au for 9Py, while for polaron 9Py + , it has increased up to 3.2 × 10 4 au. The static hyperpolarizability of the 9Py + polaronic state is 246 times higher than that of the corresponding neutral analogue, 9Py. It is observed that the values of β o obtained at the CAM-B3LYP/6-311+G(d,p) level of theory are comparable to those obtained at the LC-BLYP and ωB97XD functionals. The β vec values show a strong correlation with the total hyperpolarizability (β o ). Furthermore, the calculated second harmonic generation (SHG) values are up to 4.0 × 10 6 au at 532 nm, whereas electro-optic Pockel's effect (EOPE) is much more pronounced at the smaller dispersion frequency (1064 nm). The TD-DFT study reveal the red-shifted absorption maxima (λ max ) with an increased length of PPy + . A significant reduction in excitation energy (ΔE) is observed with increased length of PPy and PPy + , which also favors the improved NLO response. Hence, the studied thermally conducting polypyrrole-based polarons (PPy + ) are new entries into NLO materials with better electrical and optical features.

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“…PLGA, chitosan, and hyaluronic acid were the most frequently used in microneedle fabrication [ 26 , 51 , 52 ]. Several research groups have recently evaluated various materials (i.e., natural, synthetic, semisynthetic polymers, and particle composites) for microneedle fabrication [ 53 , 54 , 55 ]. Microneedles made from natural materials receive substantial attention due to their excellent compatibility and minimal skin irritation [ 56 , 57 ].…”

Section: Introductionmentioning

confidence: 99%

Microneedle-Mediated Transdermal Delivery of Biopharmaceuticals

Nguyen

2023

Pharmaceutics

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Transdermal delivery provides numerous benefits over conventional routes of administration. However, this strategy is generally limited to a few molecules with specific physicochemical properties (low molecular weight, high potency, and moderate lipophilicity) due to the barrier function of the stratum corneum layer. Researchers have developed several physical enhancement techniques to expand the applications of the transdermal field; among these, microneedle technology has recently emerged as a promising platform to deliver therapeutic agents of any size into and across the skin. Typically, hydrophilic biomolecules cannot penetrate the skin by passive diffusion. Microneedle insertion disrupts skin integrity and compromises its protective function, thus creating pathways (microchannels) for enhanced permeation of macromolecules. Microneedles not only improve stability but also enhance skin delivery of various biomolecules. Academic institutions and industrial companies have invested substantial resources in the development of microneedle systems for biopharmaceutical delivery. This review article summarizes the most recent research to provide a comprehensive discussion about microneedle-mediated delivery of macromolecules, covering various topics from the introduction of the skin, transdermal delivery, microneedles, and biopharmaceuticals (current status, conventional administration, and stability issues), to different microneedle types, clinical trials, safety and acceptability of microneedles, manufacturing and regulatory issues, and the future of microneedle technology.

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A key role by polymers in microneedle technology: a new era

Cited by 17 publications

References 157 publications

Pharmaceutical and Pharmacological Evaluation of Amoxicillin after Solubility Enhancement Using the Spray Drying Technique

Pharmaceutical and Pharmacological Evaluation of Amoxicillin after Solubility Enhancement Using the Spray Drying Technique

Polaron Formation in Conducting Polymers: A Novel Approach to Designing Materials with a Larger NLO Response

Microneedle-Mediated Transdermal Delivery of Biopharmaceuticals

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