Hydrophobically-modified gelatin hydrogel as a carrier for charged hydrophilic drugs and hydrophobic drugs

2020 ◽  
Vol 149 ◽  
pp. 140-147 ◽  
Author(s):  
Takayuki Takei ◽  
Ryosuke Yoshihara ◽  
So Danjo ◽  
Yoshiki Fukuhara ◽  
Courtney Evans ◽  
...  
Pharmaceutics ◽  
2018 ◽  
Vol 10 (3) ◽  
pp. 97 ◽  
Author(s):  
Delia Mandracchia ◽  
Adriana Trapani ◽  
Sara Perteghella ◽  
Cinzia Di Franco ◽  
Maria Torre ◽  
...  

Hydrogels are among the most common materials used in drug delivery, as polymeric micelles are too. They, preferentially, load hydrophilic and hydrophobic drugs, respectively. In this paper, we thought to combine the favorable behaviors of both hydrogels and polymeric micelles with the specific aim of delivering hydrophilic and hydrophobic drugs for dual delivery in combination therapy, in particular for colon drug delivery. Thus, we developed a hydrogel by UV crosslinking of a methacrylated (MA) amphiphilic derivative from inulin (INU) (as known INU is specifically degraded into the colon) and vitamin E (VITE), called INVITEMA. The methacrylated micelles were physicochemically characterized and subjected to UV irradiation to form what we called the “nanogrids”. The INVITEMA nanogrids were characterized by DSC, SEM, TEM, water uptake and beclomethasone dipropionate (BDP) release. In particular, the release of the hydrophobic drug was specifically assessed to verify that it can spread along the hydrophilic portions and, therefore, effectively released. These systems can open new pharmaceutical applications for known hydrogels or micelle systems, considering that in literature only few examples are present.


INDIAN DRUGS ◽  
2016 ◽  
Vol 53 (10) ◽  
pp. 16-20
Author(s):  
S. S Magdum ◽  
◽  
P.S Dounde ◽  
D. D. Kamble ◽  
S. V.* Patil ◽  
...  

Topical DDS is a localized system preferred for drugs having hurdles like first pass metabolism through gastro intestinal absorption, reduced bioavailability, relatively short residence time and dose dumping. To provide continuous percutaneous absorption of drug at controlled rate which overcomes problems associated with GI absorption for oral DDS, semisolid formulations like cream, ointment and gel were preferred in topical DDS applied on skin. Amongst them gels having more aqueous portion have greater dissolution of drug. But these properties are suitable for hydrophilic drugs and not for hydrophobic drugs. This problem was solved by formulating an emulgel in which hydrophobic drugs can be incorporated in gel and used for topical application. The aim of this work was to develop emulgel of acelofenac a hydrophobic drug using Carbapol 940 as gelling agent and clove oil and mentha oil as penetration enhancers. Another aim was to investigate effect of concentration and formulation parameters on spreading coefficient drug release and viscosity of prepared emulgel.


Author(s):  
Nicole Zoratto ◽  
Laura Forcina ◽  
Roberto Matassa ◽  
Luciana Mosca ◽  
Giuseppe Familiari ◽  
...  

The anatomy and physiology of the eye strongly limit the bioavailability of locally administered drugs. The entrapment of therapeutics into nanocarriers represents an effective strategy to topically treat some ocular disorders, as they may protect the entrapped molecules, facilitating drug residence on the ocular surface and/or its penetration into different ocular compartments. The present work shows the activity of hyaluronan-cholesterol nanogels (NHs) as ocular permeation enhancers. Thanks to their bioadhesive properties, NHs firmly interact with the superficial corneal epithelium, without penetrating the stroma, modifying the transcorneal penetration of loaded therapeutics. Ex-vivo transcorneal permeation experiments showed that the permeation of hydrophilic drugs (i.e. tobramycin and diclofenac sodium salt), loaded in NHs, is significantly enhanced when compared to the free drug solutions. On the other side the permeation of hydrophobic drugs (i.e. dexamethasone and piroxicam) is strongly dependent on the water solubility of the entrapped molecules. The obtained results suggest that NHs formulations can improve the ocular bioavailability of the instilled drugs by increasing their preocular retention time (hydrophobic drugs) or facilitating their permeation (hydrophilic drugs), thus opening the route for the application of HA-based NHs in the treatment of both anterior and posterior eye segment diseases.


Pharmaceutics ◽  
2021 ◽  
Vol 13 (11) ◽  
pp. 1781
Author(s):  
Nicole Zoratto ◽  
Laura Forcina ◽  
Roberto Matassa ◽  
Luciana Mosca ◽  
Giuseppe Familiari ◽  
...  

The anatomy and physiology of the eye strongly limit the bioavailability of locally administered drugs. The entrapment of therapeutics into nanocarriers represents an effective strategy for the topical treatment of several ocular disorders, as they may protect the embedded molecules, enabling drug residence on the ocular surface and/or its penetration into different ocular compartments. The present work shows the activity of hyaluronan-cholesterol nanogels (NHs) as ocular permeation enhancers. Thanks to their bioadhesive properties, NHs firmly interact with the superficial corneal epithelium, without penetrating the stroma, thus modifying the transcorneal penetration of loaded therapeutics. Ex vivo transcorneal permeation experiments show that the permeation of hydrophilic drugs (i.e., tobramycin and diclofenac sodium salt), loaded in NHs, is significantly enhanced when compared to the free drug solutions. On the other side, the permeation of hydrophobic drugs (i.e., dexamethasone and piroxicam) is strongly dependent on the water solubility of the entrapped molecules. The obtained results suggest that NHs formulations can improve the ocular bioavailability of the instilled drugs by increasing their preocular retention time (hydrophobic drugs) or facilitating their permeation (hydrophilic drugs), thus opening the route for the application of HA-based NHs in the treatment of both anterior and posterior eye segment diseases.


2021 ◽  
Vol 333 ◽  
pp. 11008
Author(s):  
Yoshiki Fukuhara ◽  
Yshihiro Ohzuno ◽  
Takayuki Takei ◽  
Masahiro Yoshida

Hydrogels have become popular as drug carriers. Controlled release of the drugs from hydrogels can reduce dosage, inducing prevention of side effects. However, the hydrophilicity of hydrogels interferes with controlled release of hydrophobic drugs such as anticancer agents or antibiotics. In this study, we developed hydrophobically-modified gelatin (HMG) hydrogel, which was cross-linked only by hydrophobic interaction. HMG does not require toxic chemical cross-linkers to form hydrogel. In addition, the HMG hydrogel has hydrophobic chambers in its structure which hydrophobic drugs can adsorb to and desorb from. In order to control the amount of hydrophobic drugs adsorbed into the hydrogel, hydrophobic alkyl chains with different lengths (C4-C12) were incorporated into gelatin molecules. Uranine was used as a model for hydrophobic drugs. The adsorption test exhibited that the amount of uranine adsorbed in HMG hydrogels could be controlled by varying hydrophobic alkyl chain length and that the drug could be released in a controlled manner. These results show that HMG hydrogels are promising carriers of hydrophobic drugs.


TAPPI Journal ◽  
2009 ◽  
Vol 8 (2) ◽  
pp. 33-38 ◽  
Author(s):  
ANNA JONHED ◽  
LARS JÄRNSTRÖM

The aim of this study was to investigate the properties of hydrophobically modified (HM) quaterna-ry ammonium starch ethers for paper sizing. These starches possess temperature-responsive properties; that is, gelation or phase separation occurs at a certain temperature upon cooling. This insolubility of the HM starches in water at room temperature improved their performance as sizing agents. The contact angles for water on sized liner were substantially larger than on unsized liner. When the application temperature was well above the critical phase-separation temperature, larger contact angles were obtained for liner independently of pH compared with those at the lower application temperature. Cobb60 values for liner decreased upon surface sizing, with a low pH and high application temperature giving lower water penetration. Contact angles on greaseproof paper decreased upon sur-face sizing as compared to unsized greaseproof paper, independently of pH and temperature. Greaseproof paper showed no great difference between unsized substrates and substrates sized with HM starch at different pH. This is probably due to the already hydrophobic nature of greaseproof paper. However, the Cobb60 values increased at low pH and low application temperature. Surfactants were added to investigate how they affect the sized surface. Addition of surfactant reduces the contact angles, in spite of indications of complex formation.


TAPPI Journal ◽  
2018 ◽  
Vol 17 (03) ◽  
pp. 145-153 ◽  
Author(s):  
Chengua Yu ◽  
Feng Wang ◽  
Shiyu Fu ◽  
Lucian Lucia

A very low-density oil-absorbing hydrophobic material was fabricated from cellulose nanofiber aerogels–coated silane substances. Nanocellulose aerogels (NCA) superabsorbents were prepared by freeze drying cellulose nanofibril dispersions at 0.2%, 0.5%, 0.8%, 1.0%, and 1.5% w/w. The NCA were hydrophobically modified with methyltrimethoxysilane. The surface morphology and wettability were characterized by scanning electron microscopy and static contact angle. The aerogels displayed an ultralow density (2.0–16.7 mg·cm-3), high porosity (99.9%–98.9%), and superhydrophobicity as evidenced by the contact angle of ~150° that enabled the aerogels to effectively absorb oil from an oil/water mixture. The absorption capacities of hydrophobic nanocellulose aerogels for waste engine oil and olive oil could be up to 140 g·g-1 and 179.1 g·g-1, respectively.


2019 ◽  
Author(s):  
Zihao Xu ◽  
Doh-Gyu Hwang ◽  
Michael D. Bartlett ◽  
Shan Jiang ◽  
Kaitlin M. Bratlie

Author(s):  
Neeraj Singh ◽  
Shweta Rai ◽  
Sankha Bhattacharya

Background: About two-third of new drugs reveal low solubility in water due to that; it becomes difficult for formulation scientists to develop oral solid dosage forms with a pharmaceutically acceptable range of therapeutic activity. In such cases, S-SMEEDS are the best carrier used universally for the delivery of hydrophobic drugs. SEDDS were also used, but due to its limitations, S-SMEDDS used widely. These are the isotropic mixtures of oils, co-solvents, and surfactants. S-SMEDDS are physically stable, easy to manufacture, easy to fill in gelatin capsules as well as improves the drug bioavailability by releasing the drug in the emulsion form to the gastrointestinal tract and make smooth absorption of the drug through the intestinal lymphatic pathway. Methods: We took on the various literature search related to our review, including the peer-reviewed research, and provided a conceptual framework to that. Standard tools are used for making the figures of the paper, and various search engines are used for the literature exploration.In this review article the author discussed the importance of S-SMEDDS, selection criteria for excipients, pseudo-ternary diagram, mechanism of action of S-SMEDDS, solidification techniques used for S-SMEDDS, Characterization of SEDDS and S-SMEDDS including Stability Evaluation of both and future prospect concluded through recent findings on S-SMEDDS on Cancer as well as a neoteric patent on S-SMEDDS Results: Many research papers discussed in this review article, from which it was found that the ternary phase diagram is the most crucial part of developing the SMEDDS. From the various research findings, it was found that the excipient selection is the essential step which decides the strong therapeutic effect of the formulation. The significant outcome related to solid-SMEDDS is less the globule size, higher would be the bioavailability. The adsorption of a solid carrier method is the most widely used method for the preparation of solid-SMEDDS. After review of many patents, it is observed that the solid-SMEDDS have a strong potential for targeting and treatment of a different type of Cancer due to their property to enhance permeation and increased bioavailability. Conclusion: S-SMEEDS are more acceptable pharmaceutically as compare to SEDDS due to various advantages over SEDDS viz stability issue is prevalent with SEDDS. A number of researchers had formulated S-SMEDDS of poorly soluble drugs and founded S-SMEDDS as prospective for the delivery of hydrophobic drugs for the treatment of Cancer. S-SMEEDS are grabbing attention, and the patentability on S-SMEDDS is unavoidable, these prove that S-SMEEDS are widely accepted carriers. These are used universally for the delivery of the hydrophilic drugs and anticancer drugs as it releases the drug to the gastrointestinal tract and enhances the systemic absorption. Abstract: Majority of active pharmaceutical ingredients (API) shows poor aqueous solubility, due to that drug delivery of the API to the systemic circulation becomes difficult as it has low bioavailability. The bioavailability of the hydrophobic drugs can be improved by the Self-emulsifying drug delivery system (SEDDS) but due to its various limitations, solid self-micro emulsifying drug delivery systems (S-SMEDDS) are used due to its advantages over SEDDS. S-SMEDDS plays a vital role in improving the low bioavailability of poorly aqueous soluble drugs. Hydrophobic drugs can be easily loaded in these systems and release the drug to the gastrointestinal tract in the form of fine emulsion results to In-situ solubilisation of the drug. In this review article the author's gives an overview of the solid SMEDSS along with the solidification techniques and an update on recent research and patents filled for Solid SMEDDS.


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